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)
![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) Structure](CAS/20211123/GIF/2334434-49-8.gif)
- CAS No.
- 2334434-49-8
- Chemical 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)
- Synonyms
- PF-06815345 hydrochloride;( S ) -1- ( 5- ( 4- ( 4 - ( ( 3 - chloropyridin - 2 - yl ) ( ( R ) -piperidin - 3 - yl ) carbamoyl ) -2 - fluorophenyl ) -1 - m;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)
- CBNumber:
- CB111029325
- Molecular Formula:
- C27H30Cl2FN9O4
- Molecular Weight:
- 634.49
- MDL Number:
- MOL File:
- 2334434-49-8.mol
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) Properties
| storage temp. | room temp |
|---|---|
| solubility | DMSO: 2mg/mL, clear |
| form | Solid |
| color | White to off-white |
| optical activity | [α]/D -34 to -43°, c =0.3 in methanol |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
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) Chemical Properties,Uses,Production
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.
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) Preparation Products And Raw materials
Raw materials
Preparation Products
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) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29257 | 58 |
| Merck KGaA | 21-20338288 | ordercn@merckgroup.com | China | 6394 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Merck KGaA | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 58 |
