MedKoo Cat#: 464589 | Name: CVN424
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

CVN424 is a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson’s Disease with EC50 – 38 nM. CVN424 is brain-penetrant and shows dose-dependent receptor occupancy that attained brain 50% of receptor occupancy at plasma concentrations of 6.0 and 7.4 ng/ml in mice and rats, respectively. Oral administration of CVN424 dose-dependently increases locomotor activity and reverses haloperidol-induced catalepsy. Furthermore, CVN424 restored mobility in bilateral 6-hydroxydopamine lesion model of Parkinson disease.

Chemical Structure

CVN424
CVN424
CAS#2254706-21-1

Theoretical Analysis

MedKoo Cat#: 464589

Name: CVN424

CAS#: 2254706-21-1

Chemical Formula: C25H31F2N5O2

Exact Mass: 471.2446

Molecular Weight: 471.55

Elemental Analysis: C, 63.68; H, 6.63; F, 8.06; N, 14.85; O, 6.79

Price and Availability

Size Price Availability Quantity
5mg USD 650.00 2 Weeks
10mg USD 1,050.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
CVN424; CVN 424; CVN-424; Solangepras
IUPAC/Chemical Name
(R)-2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-6-(prop-1-en-2-yl)-N-(tetrahydrofuran-3-yl)-5,6,7,8-tetrahydropyrido[3,4-b]pyrazin-3-amine
InChi Key
OJQWTBAKFUKZFP-GOSISDBHSA-N
InChi Code
InChI=1S/C25H31F2N5O2/c1-16(2)32-11-7-21-22(14-32)29-24(28-18-8-12-33-15-18)25(30-21)31-9-5-19(6-10-31)34-23-4-3-17(26)13-20(23)27/h3-4,13,18-19H,1,5-12,14-15H2,2H3,(H,28,29)/t18-/m1/s1
SMILES Code
FC1=C(OC2CCN(C3=NC4=C(CN(C(C)=C)CC4)N=C3N[C@H]5COCC5)CC2)C=CC(F)=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 471.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Sun H, Monenschein H, Schiffer HH, Reichard HA, Kikuchi S, Hopkins M, Macklin TK, Hitchcock S, Adams M, Green J, Brown J, Murphy ST, Kaushal N, Collia DR, Moore S, Ray WJ, Carlton MBL, Brice NL. First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. J Med Chem. 2021 Apr 16. doi: 10.1021/acs.jmedchem.0c02081. Epub ahead of print. PMID: 33861086. 2: Brice NL, Schiffer HH, Monenschein H, Mulligan VJ, Page K, Powell J, Xu X, Cheung T, Burley JR, Sun H, Dickson L, Murphy ST, Kaushal N, Sheardown S, Lawrence J, Chen Y, Bartkowski D, Kanta A, Russo J, Hosea N, Dawson LA, Hitchcock SH, Carlton MB. Development of CVN424: a selective and novel GPR6 inverse agonist effective in models of Parkinson's Disease. J Pharmacol Exp Ther. 2021 Apr 1:JPET-AR-2020-000438. doi: 10.1124/jpet.120.000438. Epub ahead of print. PMID: 33795395.