| Identification | Back Directory | [Name]
Carbonic acid, (1S)-1-[5-[4-[4-[[(3-chloro-2-pyridinyl)(3R)-3-piperidinylamino]carbonyl]-2-fluorophenyl]-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl]ethyl ethyl ester, hydrochloride (1:1) | [CAS]
2334434-49-8 | [Synonyms]
Carbonic acid, (1S)-1-[5-[4-[4-[[(3-chloro-2-pyridinyl)(3R)-3-piperidinylamino]carbonyl]-2-fluorophenyl]-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl]ethyl ethyl ester, hydrochloride (1:1) | [Molecular Formula]
C27H30Cl2FN9O4 | [MOL File]
2334434-49-8.mol | [Molecular Weight]
634.49 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [color ]
White to off-white | [Optical Rotation]
[α]/D -34 to -43°, c =0.3 in methanol |
| Hazard Information | Back Directory | [Description]
PF-06815345 HCl is a liver-targeted, orally available prodrug. | [Uses]
PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse[1][2]. | [in vivo]
PF-06815345 hydrochloride (Example 7) (100-500 mg/kg; p.o; single dose) lowers the level of PCSK9 in humanized PCSK9 mouse model. It lowers plasma PCSK9 to 72% at 500 mg/kg 4 hr later treatment[2].
| [References]
[1] Akin A, et al. Overcoming the Challenges of Making a Single Enantiomer N-1 Substituted Tetrazole Prodrug Using a Tin-Mediated Alkylation and Enzymatic Resolution[J]. Organic Process Research & Development, 2019, 23(6): 1167-1177.
[2] Darout E, et al. Preparation of substituted amide compounds as PCSK9 inhibitors: Canada, CA2907071 A1 2016-04-08. |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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