N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-
BIIE 0246
CAS: 246146-55-4
Molecular Formula: C49H57N11O6
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1- - Names and Identifiers
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1- - Physico-chemical Properties
| Molecular Formula | C49H57N11O6 |
| Molar Mass | 896.05 |
| Density | 1.38±0.1 g/cm3(Predicted) |
| pKa | 13.28±0.40(Predicted) |
| Storage Condition | Store at +4°C |
| In vitro study | Receptor binding assays in HEK 293 cells transfected with the rat Y2 receptor cDNA demonstrate that BIIE-0246 competes with high affinity (IC 50 =15±3 nM) against specific [ 125 I]PYY 3-36 binding sites. In contrast, BIIE-0246, at concentrations up to 10 μM, fails to compete for significant amounts of specific [ 125 I]GR231118, [ 125 I]hPP and [ 125 I][Leu 31 , Pro 34 ]PYY binding sites in HEK 293 cells transfected with the rat Y 1 , Y 4 or Y 5 receptor cDNA, respectively. |
| In vivo study | On chow diet, genetically obese NPY mice show increased gain in body weight and adiposity. Treatment with BIIE-0246 promotes body weight gain in both genotypes after 4.5 weeks, and already at 2 weeks. BIIE-0246 has no significant effect on fat mass gain. In DIO, BIIE-0246 has different effects on body weight and composition depending on the genotype (treatment×genotype interaction in body weight P<0.05, in fat mass P<0.001 and in lean mass P<0.05). In DIO-WT group, post hoc analysis reveals increased body weight and fat mass gain, and a tendency to decrease lean mass gain. In DIO-NPY, BIIE-0246 inhibits fat mass gain (P=0.05). Interestingly, increased cholesterol levels are detected also in WT mice treated with BIIE-0246 for 2 weeks, but not in the 4.5-week cohort. In DIO-NPY mice in both treatment groups, cholesterol levels correlate positively with body fat mass (DIO-NPY vehicle P<0.01; DIO-NPY BIIE-0246 P<0.001), but not in any other group, and the slope of the regression curve of cholesterol and fat mass is significantly decreased in BIIE-0246-treated DIO-NPY group when compared with vehicle-treated group. |
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1- - Introduction
BIIE 0246 (full name BIIE-0246 hydrochloride) is a chemical substance with the chemical name 2-amino-4, 5-dimethy1-3-thienyl-[3-(trifluoromethyl)phenyl]methanone hydrochloride. The following is a description of the nature, use, formulation and safety information of BIIE 0246:
Nature:
-Appearance: BIIE 0246 is a white to off-white crystal powder.
-Solubility: It is soluble in polar solvents such as water, methanol and DMSO (dimethyl sulfoxide).
Use:
- BIIE 0246 is a chemical substance, mainly used in the field of scientific research. It is A GABA (gamma-aminobutyric acid) A receptor antagonist. The GABA A receptor is A neurotransmitter receptor, and the study of the BIIE 0246 helps to study neurotransmission and synaptic function.
Preparation Method:
The preparation method of-BIIE 0246 is mainly realized by chemical synthesis, and the specific preparation steps are usually operated by professional chemical researchers in the laboratory.
Safety Information:
-For the use of any chemical substance, safety is of paramount importance. Since BIIE 0246 is a chemical used in professional research, it is essential to understand and follow the safety information. The following is general safety information:
- BIIE 0246 is irritating and dangerous, and should be kept away from fire and high temperature.
-observe personal protective measures such as gloves, goggles and protective clothing when contacting BIIE 0246.
-in the use, storage and handling of BIIE 0246, should follow the relevant safety procedures and laboratory safety guidelines.
-Avoid direct inhalation or contact with skin and eyes. In case of accidental contact, rinse immediately with water and seek medical help.
-When using or handling BIIE 0246, appropriate waste disposal methods and environmental protection regulations should be followed.
Please note that this information is for informational purposes only. Before using and handling any chemical substances, it is recommended to consult the detailed technical data and safety instructions provided by the supplier to ensure safe operation and appropriate environmental protection measures.
Nature:
-Appearance: BIIE 0246 is a white to off-white crystal powder.
-Solubility: It is soluble in polar solvents such as water, methanol and DMSO (dimethyl sulfoxide).
Use:
- BIIE 0246 is a chemical substance, mainly used in the field of scientific research. It is A GABA (gamma-aminobutyric acid) A receptor antagonist. The GABA A receptor is A neurotransmitter receptor, and the study of the BIIE 0246 helps to study neurotransmission and synaptic function.
Preparation Method:
The preparation method of-BIIE 0246 is mainly realized by chemical synthesis, and the specific preparation steps are usually operated by professional chemical researchers in the laboratory.
Safety Information:
-For the use of any chemical substance, safety is of paramount importance. Since BIIE 0246 is a chemical used in professional research, it is essential to understand and follow the safety information. The following is general safety information:
- BIIE 0246 is irritating and dangerous, and should be kept away from fire and high temperature.
-observe personal protective measures such as gloves, goggles and protective clothing when contacting BIIE 0246.
-in the use, storage and handling of BIIE 0246, should follow the relevant safety procedures and laboratory safety guidelines.
-Avoid direct inhalation or contact with skin and eyes. In case of accidental contact, rinse immediately with water and seek medical help.
-When using or handling BIIE 0246, appropriate waste disposal methods and environmental protection regulations should be followed.
Please note that this information is for informational purposes only. Before using and handling any chemical substances, it is recommended to consult the detailed technical data and safety instructions provided by the supplier to ensure safe operation and appropriate environmental protection measures.
Last Update：2024-04-09 21:04:16
![N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-](http://res.chembk.com/assets/images/structure/246146-55-4.gif)
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Product Name: BIIE-0246 Visit Supplier Webpage Request for quotationCAS: 246146-55-4
Tel: +86-400-900-4166
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Mobile: +86-18621343501
QQ: 2881950922
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Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
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Product Name: BIIE 0246 Visit Supplier Webpage Request for quotation
CAS: 246146-55-4
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CAS: 246146-55-4
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View History
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-
30240-13-2
1-methyl-1-ethyl-4-oxopiperidinium iodide
2243125-98-4
56539-66-3
(S)-2-[[(2R,4S,5S)-5-(tert-Butoxycarbonylamino)-2-benzyl-4-hydroxy-6-phenylhexanoyl]amino]-3-cyclohexylpropionamide
N-Phenyl-8-naphthylamine-1-sulfonic acid
76-66-4
586992-12-3
1354488-21-3
30240-13-2
1-methyl-1-ethyl-4-oxopiperidinium iodide
2243125-98-4
56539-66-3
(S)-2-[[(2R,4S,5S)-5-(tert-Butoxycarbonylamino)-2-benzyl-4-hydroxy-6-phenylhexanoyl]amino]-3-cyclohexylpropionamide
N-Phenyl-8-naphthylamine-1-sulfonic acid
76-66-4
586992-12-3
1354488-21-3