坎格雷洛四钠盐 3级
cangrelor tetrasodium
CAS: 163706-36-3
Molecular Formula: C17H21Cl2F3N5Na4O12P3S2
坎格雷洛四钠盐 3级 - Names and Identifiers
| Name | cangrelor tetrasodium |
| Synonyms | CS-1027 angrelor tetrasodium cangrelor tetrasodium CANGRELOR TETRASODIUM SALT Cangrelor Tetrasodium Salt AR-C 69931 Tetrasodium Salt N-[2-(Methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]adenosine-5'-O-(β,γ-dichloromethylene)triphosphate tetrasodium salt tetrasodium 5'-O-[({[dichloro(phosphonato)methyl]phosphinato}oxy)phosphinato]-N-[2-(methylsulfanyl)ethyl]-2-[(3,3,3-trifluoropropyl)sulfanyl]adenosine |
| CAS | 163706-36-3 |
| EINECS | 813-784-1 |
坎格雷洛四钠盐 3级 - Physico-chemical Properties
| Molecular Formula | C17H21Cl2F3N5Na4O12P3S2 |
| Molar Mass | 864.2865126 |
| Storage Condition | 2-8℃ |
| Use | Cangrelor is an ATP analog that inhibits platelet aggregation (IC50 = 0.4 nM). It is a reversible competitive antagonist of the platelet purinergic P2Y12 receptor. Pretreatment with cangrelor significantly reduces blood clotting induced by ADP in a mouse model of pulmonary thromboembolism. Formulations containing cangrelor have been used to prevent blood clotting in at-risk patients. |
坎格雷洛四钠盐 3级 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.157 ml | 5.785 ml | 11.57 ml |
| 5 mM | 0.231 ml | 1.157 ml | 2.314 ml |
| 10 mM | 0.116 ml | 0.579 ml | 1.157 ml |
| 5 mM | 0.023 ml | 0.116 ml | 0.231 ml |
Last Update：2024-01-02 23:10:35
坎格雷洛四钠盐 3级 - Reference Information
| Use | kangrelor (code: AR-C69931MX) it is a non-thienopyridine direct acting P2Y12 receptor antagonist, which can be used for the treatment of acute coronary syndrome (ACS), and can also be used as a rapid-acting anti-thrombotic drug for intravenous injection. Cangrel can rapidly inhibit platelet aggregation, and can produce activity in the body without metabolism. In vitro experiments found that cangrel can reduce the platelet-leukocyte reaction in the blood of patients with ACS, indicating that the drug may also have disease improvement function. Phase II clinical studies have shown that the anti-platelet aggregation effect of kangrelor is stronger than that of clopidogrel, and has good safety. A p2y12 inhibitor that almost completely inhibits ADP-induced platelet aggregation. Cangrelor is a P2Y12 inhibitor.Cangrelor is a high-affinity, reversible inhibitor of P2Y12 receptors that causes almost complete inhibition of ADP-induced platelet aggregate. It is a modified ATP derivative stable to enzymatic degradation. It does not require metabolic conversion to an active metabolite. This allows cangrelor's immediate effect after infusion, and the therapeutic effects can be maintained with continuous infusion. |
| pharmacological effects | platelets have 3 kinds of adenine nucleotide P2 receptors, including P2Y1, P2Y12, P2X1, p2Y12 interacts with adenosine diphosphate (ADP) and P2X1 interacts with adenosine triphosphate (ATP). Kangrelor binds directly to the P2Y12 receptor in vivo without being metabolized. In vitro wash platelet nephelometry analysis showed that canaglio inhibited ADP(30mmol • L-1)-induced platelet aggregation with a pIC50 (half inhibitory concentration against value) of 9.4. In whole blood, the anti-platelet aggregation activity of kangrelor varies according to the measurement method, and heparinized blood samples (induced at 3mmol L-1ADP) are measured by impedance aggregometry, pIC50 was determined to be 9.2 for kangrello, whereas pIC50 was determined to be 7.6 for citrate blood samples (induced at 20mmol • L-1ADP) by platelet residue counting. Different experimental results may be related to the concentration of ADP in the sample fluid, the degree of blood dilution or the type of anticoagulant. In addition, in the blood of other species of animals, the product also showed strong anti-platelet aggregation activity, the pIC50 in the heparin-added dog and rat blood samples was 9.2 and 8.3, respectively, as determined by impedance aggregometry. By inhibiting the P2Y12 receptor, cangrel can produce significant anti-platelet aggregation activity, while also partially inhibiting the intracellular Ca2 concentration, both of which can be affected by prostaglandin E1(PGE1). PGI2 is enhanced by activating adenylate cyclase to increase cAMP levels in vivo. In addition, the product can interfere with the sustained activation of gpIIb/IIIa receptors induced by potent platelet agonists such as thrombin by inhibiting Rap-1b instead of protein kinase C(PKC). Kangrelor not only reduces thrombin-induced platelet activation, but also produces a synergistic effect with the thrombin inhibitor melagatran. Under the high shear force, the pre-cultured blood with kangrello can reduce the binding force of platelets and immobilized von Willebrand factor, and the transient interaction is not affected. |
| pharmacokinetics and metabolism | as mentioned earlier, kangrelor can antagonize P2Y12 receptor without being metabolized, and because of its structure containing triphosphate side chain, so the goods in vivo half-life is short, only 2.6min, plasma clearance rate of 50L • h-1. The short half-life makes cangrel an ideal anti-platelet aggregation drug for intravenous injection. The tissue distribution of kangrelor in rats was determined by autoradiography. The results showed that its distribution in vivo was limited to plasma due to its physical and chemical properties. After instillation of 3H-labeled cangrilo into male rats, the heart, lung, liver, spleen and other vascular-rich parts of the rats showed high radioactivity, but then decreased rapidly, and then distributed to the liver, kidney, intestine and other metabolic organs. This product has no distribution in the central nervous system. |
| biological activity | cancrelor (AR-C69931MX) is a potent, competitive inhibitor of P2Y12 receptor, inhibits ADP-induced platelet aggregation. |
| Target | Value |
Last Update：2024-04-10 22:41:03
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View History
坎格雷洛四钠盐 3级
2-甲基-beta-萘并噻唑
GOSERELIN ACETATE 醋酸戈舍瑞林及杂质对照品
(S)-苄基2-((((9H-芴-9-基)甲氧基)羰基)氨基)-5-羟基戊酸酯
乙炔基苯基碘鎓四氟硼酸盐[乙炔基化试剂]
2-甲基-beta-萘并噻唑
GOSERELIN ACETATE 醋酸戈舍瑞林及杂质对照品
(S)-苄基2-((((9H-芴-9-基)甲氧基)羰基)氨基)-5-羟基戊酸酯
乙炔基苯基碘鎓四氟硼酸盐[乙炔基化试剂]