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| Cas No.: | 170151-24-3 |
| Chemical Name: | Nepicastat HCl |
| Synonyms: | SYN117; SYN-117; SYN 117; RS25560197; RS25560-197; RS-25560-197; RS 25560-197; Nepicastat; Nepicastat HCl |
| SMILES: | C1CC2=C(C=C(C=C2C[C@H]1N3C(=CNC3=S)CN)F)F.Cl |
| Formula: | C14H15F2N3S |
| M.Wt: | 295.35 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Nepicastat Hcl(SYN117 Hcl; RS-25560-197 Hcl) is a dopamine beta-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively.Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat (SYN117; RS-25560-197) has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such. |
| Target: | IC50 value: 8.5/9.0 nM(bovine/human dopamine beta-hydroxylase) |
| References: | [1]. Stanley WC, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.Br J Pharmacol. 1997 Aug;121(8):1803-9. [2]. Stanley WC, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor.J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70. [3]. Sabbah HN, et al. Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.Circulation. 2000 Oct 17;102(16):1990-5. [4]. Beliaev A, et al. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase.J Med Chem. 2006 Feb 9;49(3):1191-7. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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