18883-66-4 - Names and Identifiers
Name | Streptozocin
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Synonyms | STZ STR STREPTOZOCIN Streptozocin STREPTOZOTOCIN Streptozotocin Streptozotocin (U-9889) N-(METHYLNITROSOCARBAMOYL)-A-D-GLUCOSAMINE N-(METHYLNITROSOCARBAMOYL)-ALPHA-GLUCOSAMINE N-(METHYLNITROSOCARBAMOYL)-ALPHA-D-GLUCOSAMINE 2-desoxy-2-(3-methyl-3-nitrosoureido)-d-glucopyranose 2-deoxy-2-(((methylnitrosoamino)carbonyl)amino)-d-glucose 2-deoxy-2-{[methyl(nitroso)carbamoyl]amino}-D-glucopyranose 2-deoxy-2-{[methyl(nitroso)carbamoyl]amino}-beta-D-glucopyranose 2-deoxy-2-{[methyl(nitroso)carbamoyl]amino}-alpha-D-glucopyranose (5xi)-2-deoxy-2-{[methyl(nitroso)carbamoyl]amino}-D-lyxo-hexopyranose
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CAS | 18883-66-4
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EINECS | 242-646-8 |
InChI | InChI=1/C8H15N3O7/c1-11(10-17)8(16)9-4-6(14)5(13)3(2-12)18-7(4)15/h3-7,12-15H,2H2,1H3,(H,9,16)/t3-,4-,5-,6-,7-/m1/s1 |
InChIKey | ZSJLQEPLLKMAKR-FEQHFJGESA-N |
18883-66-4 - Physico-chemical Properties
Molecular Formula | C8H15N3O7
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Molar Mass | 265.22 |
Density | 1.4410 (rough estimate) |
Melting Point | 121 °C (dec.) (lit.) |
Boling Point | 408.44°C (rough estimate) |
Specific Rotation(α) | D25 +39° |
Water Solubility | soluble |
Solubility | 53 mg/mL soluble in water and DMSO, insoluble in ethanol. However, its aqueous solution is extremely unstable at room temperature and can be decomposed into gas and volatilized after half an hour, so it needs to be used now. |
Appearance | Pale yellow crystalline powder |
Color | white to light yellow |
Merck | 13,8912 |
BRN | 2060675 |
pKa | pKa 1.3 (Uncertain) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 1 month. |
Sensitive | Hygroscopic |
Refractive Index | 1.6500 (estimate) |
MDL | MFCD00006607 |
Physical and Chemical Properties | Melting point 115°C (dec.) water-soluble soluble
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Use | This product is for scientific research only and shall not be used for other purposes. |
In vitro study | Streptozotocin directly alkylates DNA and is highly genotoxic, producing DNA strand damage, base-labile sites, extra-period DNA synthesis, DNA adducts, chromosomal aberrations, micronuclei, sister Chromatid Exchange, and cell death. Free radicals are involved in the synthesis of DNA and chromosomes are destroyed by Streptozotocin. |
In vivo study | Streptozotocin is often used to induce diabetes in animal experiments. Streptozotocin selectively accumulates in pancreatic islet β-cells by the low-affinity GLUT 2 glucose transporter. A 4-month injection of Streptozotocin (60 mg/kg) induced rapid degranulation of β-cells without necrosis, cataract development, and glycogen accumulation in the proximal convoluted tubules of the kidney. In 'streptozotocin diabetes' rats, Streptozotocin (100 mg/kg) caused damage to pancreatic exocrine cells, allowing small, potentially secretory granules to persist in the Golgi apparatus of beta cells. Streptozotocin has been found to be carcinogenic in rats, mice and hamsters. The administration of Streptozotocin alone was able to induce tumors in the kidney, liver, lung, pancreas, and uterus of hamsters. Intraperitoneal administration of Streptozotocin (100-150 mg/kg) to normotensive Wistar Kyoto rats (WKY) for 12 months induced carcinogenesis, with a 70% tumor incidence in the liver, the incidence of tumors in the kidney is 20%, and there is a 10% possibility of simultaneous liver and kidney lesions. |
18883-66-4 - Risk and Safety
Risk Codes | R40 - Limited evidence of a carcinogenic effect
R61 - May cause harm to the unborn child
R46 - May cause heritable genetic damage
R45 - May cause cancer
R22 - Harmful if swallowed
R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed.
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Safety Description | S36/37 - Wear suitable protective clothing and gloves.
S53 - Avoid exposure - obtain special instructions before use.
S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.)
S36 - Wear suitable protective clothing.
S22 - Do not breathe dust.
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UN IDs | 3249 |
WGK Germany | 3 |
RTECS | LZ5775000 |
FLUKA BRAND F CODES | 3-10-21 |
HS Code | 29419090 |
Hazard Class | 6.1(b) |
Packing Group | III |
Toxicity | LD50 in female mice (mg/kg): 360 i.p.; 275 i.v.; in male dogs (mg/kg): 50 i.v. (Iwasaki) |
18883-66-4 - Introduction
Biological activity: This product is a nitrosourea antibiotic, mainly used for insulin cell carcinoma (β cell or non-β cell carcinoma), and has a certain effect on carcinoid tumors, Hodgkin's disease, colon cancer and liver cancer. It is an effective DNA methylation reagent, acting on HL60,K562 and C1498 cells with IC50 of 11.7,904 and 1024 μg/mL respectively. The laboratory is often used to replicate diabetes models. Description: This product is Stre.achromogenes Uar. The nitrosourea antibiotics produced by 128 are different from fat-soluble nitrosourea. It is a methyl group at the chloroethyl group and an amino sugar at the other end of the molecule. STZ can decompose the active methyl n-carbon ions by itself and cross-link with DNA between strands, thereby alkylating DNA, but its alkylation is weaker than other nitrosourea drugs, and its metabolite methyl nitrosourea The alkylation effect is 3-4 times stronger than its STZ. STZ can form isocyanate in vivo. So as to combine with nucleic acid protein, inhibit DNA polymerase activity, and make damaged DNA difficult to repair. In the process of anti-tumor research, it was found that STZ can increase the blood sugar of mice, and it can cause diabetes in dogs and monkeys, and it is permanent. The diabetic effect of STZ has species difference, which is not caused in guinea pigs or in humans. The mechanism of diabetes is mainly due to the decrease of nicotinamide adenine (DNA) content in islet cells, and the glucose group in STZ molecule can make STZ enter islet β cells, causing morphological changes in β cell nucleus, causing chromosome agglutination, elongation and concentration. Use method recommendation (for reference only) Take the diabetes model as an example to illustrate the use of STZ. 1. Prepare citric acid buffer solution A: weigh 2.1g of citric acid (MW:210.14) and add 100 mL of double distilled water to prepare solution A; Liquid B: 2.94g of sodium citrate (MW:294.10) is added into 100 mL of double distilled water to prepare liquid B. Mix liquid A and liquid B according to a certain proportion (1:1.32 is also 1:1), measure the pH value, and adjust the pH value in the range of 4.2-4.5, which is the citric acid buffer solution for STZ. 2. Before preparing STZ injection before injection, STZ is placed in a dry sterilization bottle, wrapped with tin foil for the outside, pre-cooled in an ice bath together with citric acid buffer, and brought to the animal room for later use. 3. Rats prepared with injection were weighed after overnight fasting. Rats were grouped in order to dissolve STZ according to the grouping. According to fasting body weight, 1% STZ injection was prepared with citric acid buffer. If the subsequent injection operation is not skilled, do not dissolve STZ at one time. Note: STZ is easy to deactivate. After STZ is quickly weighed, it is still required to dry and avoid light. It is recommended to use dry aluminum foil (or tin foil) paper. 4. Intraperitoneal injection or tail vein injection. If the injection operation technique is not skilled, the two groups should be injected alternately and the injection is completed within 30 minutes. Note: Most injections require rapid injections. FAQ 1. Q: How to store STZ powder after receiving it? Answer: After packaging, seal the bottle mouth with sealing film, wrap the bottle with aluminum foil (or tinfoil, that is, avoid light), put it in a drying tank (desiccant, that is, keep dry), and refrigerate at -20 ℃, which can be stored for a long time. 2. Question: Why do rats fast before modeling? Answer: Fasting for more than 12 hours (usually fasting overnight, water is not needed). The longer the fasting time, the more obvious the destructive power of STZ to islet β cells, that is, the higher the drug effect. Therefore, the relative fasting time is prolonged, which can reduce the dosage of STZ. 3. Q: When modeling, the dosage of STZ is commonly used? Answer: Taking the average weight of 200 grams of mice as an example, type I diabetes model: the dose of rats is 70~65 mg/kg; Type II diabetes model: rats fed with high sugar and high fat for 1~2 months, the dose of STZ is 25~40 mg/kg; Or references. This dose is for reference only. It is recommended to explore the optimal dose through pre-experiments. 4. Q: Is pre-experiment very important? A: Very important. During the experiment, the dosage of STZ should refer to the results of the pre-experiment, and try not to blindly use it directly according to the dosage of the literature or others. The mice are both heavy and fasting (low sugar state) drug resistance, fasting time, injection and selection, as well as the previous feeding process, sugar measurement and selection, etc. It is the most scientific to determine the dosage that conforms to the experimental mice through pre-experiment. 5. Q: How does the injection method affect the experimental results? Answer: Tail injection is intravenous injection, and the drug utilization rate is relatively high. Compared with intraperitoneal injection, it can save the amount of medicine. The disadvantage is that it is not as convenient as intraperitoneal injection. 6. Q: What is the relationship between advancing speed and blood sugar during injection? Answer: The speed of bolus injection is fast, and it is easier to form hyperglycemia. The speed of bolus injection is slow, and the relative risk is relatively low, but it is not easy to form a mold. In routine operations, rapid injection is often required. Of course, the dose of STZ is the main factor that determines the level of blood sugar. 7. Q: Is it normal for rats to die after STZ injection? How to solve it? Answer: Normal. Individual differences in mice and differences in fasting (hypoglycemia) resistance lead to different mortality rates. The initial high mortality rate may be mainly due to sudden increase in blood sugar, maladjustment in mice, or DKA (ie ketoacidosis). First of all, we must ensure sufficient drinking water (insufficient drinking water can easily lead to dead rats). Secondly, both hyperglycemia and hypoglycemia can cause dead rats. Avoiding dead rats can be done by injecting insulin or temporarily supplementing sugar. Way 1: Insulin supplement method. The common cause of death is high blood sugar. It can be supplemented with some moderate-effect insulin (such as novolin n or NPH (neutral protamine zinc insulin)), 2-3 units at a time, and after 3-5 days, the mortality rate of rats is usually reduced. Way 2: sugar supplement method. Rats after fasting were already in a state of hypoglycemia at the time of injection. Intraperitoneal injection of 20% glucose 4 hours after modeling can prevent rats from dying due to low blood sugar during injection. Again, prevent animals from killing each other. In the case of lack of food and insufficient water supply, they will tear each other and eat the same kind. Therefore, food and drinking water should be provided in sufficient supply, preferably in two ways. Finally, prevent infection. Diabetic rats have a lot of urine and wet padding, so they need to change the padding frequently. Therefore, diabetic rats are more prone to infection than other rats, especially urinary tract infection and abdominal infection. Before and after invasive operations such as intraperitoneal injection, subcutaneous injection and blood sampling for blood glucose measurement, attention should be paid to disinfection. For example, tetracycline (or chlortetracycline eye ointment) can be applied locally after each blood collection to measure blood sugar to prevent infection. 8. Question: After the injection of STZ, the model is unsuccessful, how to deal with it? Answer: If the model fails to meet the standard, it is easy to inject STZ (intraperitoneal injection at a dose of 10 mg-20 mg/kg body weight) three days later, and it is also easy to form a model, or after the blood sugar returns to normal, the conventional dose is injected; but to achieve the desired effect, it is often to return to the normal state to re-model. [Note] ● STZ is unstable due to damp. If it needs to be weighed many times, it should be operated and stored in strict accordance with the principle of avoiding damp. The operating environment, containing containers, and sub-packaging tools must be kept dry. ● Long-term exposure should be avoided to prevent moisture and failure 30 minutes after moisture. This is the same as the requirement for rapid injection during modeling, that is, its aqueous solution is unstable. ● Injection is only formulated before injection because STZ aqueous solution is extremely unstable.
Last Update:2022-10-16 17:14:38