857347 | VPC 51299

(R,E)-(3-palmitamido-4-(4-((4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methoxy)phenyl)but-1-en-1-yl)phosphonic acid


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VPC 51299

VPC 51299

(R,E)-(3-palmitamido-4-(4-((4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methoxy)phenyl)but-1-en-1-yl)phosphonic acid

VPC51299 is a potent low micromolar inhibitor containing a vinyl phosphonate head group and possessing a half-life of approximately 90 min in rats when dosed intravenously. Previously developed LPA1/LPA3 receptor antagonists contain a labile phosphate head group which impairs evaluation of scaffold LPA receptor antagonists in vivo. VPC51299 has replaced the phosphate with a more stable head group while retaining potency at both LPA1 and LPA3 to facilitate future in vivo studies of the biological functions of these receptors.
Refer: J.E. East, et al. (2011). Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm 2:325-330.

This product is covered by Patent Number US 8,283,339 B2. Avanti manufactures this under license from University of Virginia.

Hygroscopic
Yes
Light Sensitive
No
Molecular Formula
C34H50 F3N2O6P
Percent Composition
C 60.88%, H 7.51%, F 8.50%, N 4.18%, O 14.31%, P 4.62%
Purity
>99%
Stability
1 Years
Storage Temperature
-20°C
CAS Number
1004787-61-4
CAS Registry Number is a Registered Trademark of the American Chemical Society
Formula Weight
670.740
Exact Mass
670.336

East JE, Carter KM, Kennedy PC, Schulte NA, Toews ML, Lynch KR, Macdonald TL. Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm. 2011 Mar 3;2(4):325-330. doi: 10.1039/C0MD00273A. PMID: 22180836; PMCID: PMC3237054.

PubMed ID: 22180836