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PF-06815345

Names

[ CAS No. ]:
1900686-46-5

[ Name ]:
PF-06815345

[Synonym ]:
(1S)-1-{5-[4-(4-{(3-Chloro-2-pyridinyl)[(3R)-3-piperidinyl]carbamoyl}-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl}ethyl ethyl carbonate
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

Biological Activity

[Description]:

PF-06815345 (PF 6815345) is a potent prodrug PCSK9 modulator that inhibits PCSK9 secretion in vitro translation assay; PF-06815345is identified after optimization of the prodrug moiety to maximize intestinal stability achieving liver targeting of the active compound after prodrug turnover by carboxylesterase (CES1). Hypercholesterolemia Phase 1 Discontinued

[References]

References 1. McClure KF, et al. Angew Chem Int Ed Engl. 2017 Dec 18;56(51):16218-16222. 2. Daniel Pettersen, et al. Small molecule modulators of PCSK9-a literature and patent overview. Bioorg Med Chem Lett. 2018 Feb 26. pii: S0960-894X(18)30151-3. View Related Products by Target PCSK9 Hypercholesterolemia

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
775.4±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H29ClFN9O4

[ Molecular Weight ]:
598.029

[ Flash Point ]:
422.7±35.7 °C

[ Exact Mass ]:
597.201477

[ LogP ]:
2.13

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.686

Related Compounds