SSR240612
Cat. No.：YN320942
CAS No. ：464930-42-5
| 产品名称: | SSR240612 |
| CAS No.: | 464930-42-5 |
| Chemical Name: | (3R)-3-(1,3-benzodioxol-5-yl)-N-[(6-methoxy-2-naphthalenyl)sulfonyl]-β-alanyl-4-[[(2R,6S)-2,6-dimethyl-1-piperidinyl]methyl]-N-methyl-N-(1-methylethyl)-D-phenylalaninamide, monohydrochloride |
| Synonyms: | SSR-240612; SSR240612; SSR 240612 |
| 分子量: | 793.41 |
| 分子式: | C₄₂H₅₃ClN₄O₇S |
| SMILES: | O=S(N[C@@H](C1=CC=C2C(OCO2)=C1)CC(N[C@@H](C(N(C)C(C)C)=O)CC3=CC=C(CN([C@@H]4C)[C@H](CCC4)C)C=C3)=O)(C5=CC(C=CC(OC)=C6)=C6C=C5)=O.Cl[H] |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | SSR240612 是一种有效的，可口服的，特异性的非肽类缓激肽 B1 (bradykinin B1) 受体拮抗剂，对bradykinin B1受体（在人 MRC5 细胞和表达人 B1 受体的 HEK 细胞）的Ki值分别为 0.48 nM，0.73 nM；对 B2 受体 (在豚鼠回肠膜和表达人 B1 受体的 CHO 细胞) 的Ki较弱，分别为 481 nM 和 358 nM。 |
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Gougat, J., Ferrari, B., Sarran, L., et al.SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist of the bradykinin B1 receptor: Biochemical and pharmacological characterizationJ. Pharmacol. Exp. Ther.309(2),661-669(2004)
Huart, A., Klein, J., Gonzalez, J., et al.Kinin B1 receptor antagonism is equally efficient as angiotensin receptor 1 antagonism in reducing renal fibrosis in experimental obstructive nephropathy, but is not additiveFront. Pharmacol.6:8,(2015)
De Brito Gariepy, H., Carayon, P., Ferrari, B., et al.Contribution of the central dopaminergic system in the anti-hypertensive effect of kinin B1 receptor antagonists in two rat models of hypertensionNeuropeptides44(2),191-198(2010)
Dias, J.P., and Couture, R.Blockade of kinin B1 receptor reverses plasma fatty acids composition changes and body and tissue fat gain in a rat model of insulin resistanceDiabetes Obes. Metab.14(3),244-253(2012)
