Description
AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response.
Product information
CAS Number: 2250019-94-2
Molecular Weight: 529.05
Formula: C26H29ClN4O4S
Chemical Name: 5-[(3R)-3-hydroxypyrrolidine-1-carbonyl]-3-methyl-1-(2-methylpropyl)-6-[(quinolin-4-yl)methyl]-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione hydrochloride
Smiles: Cl.CN1C(=O)N(CC(C)C)C2SC(CC3=CC=NC4=CC=CC=C34)=C(C=2C1=O)C(=O)N1C[C@H](O)CC1
InChiKey: NFFGLQDNUHBVEY-UNTBIKODSA-N
InChi: InChI=1S/C26H28N4O4S.ClH/c1-15(2)13-30-25-22(23(32)28(3)26(30)34)21(24(33)29-11-9-17(31)14-29)20(35-25)12-16-8-10-27-19-7-5-4-6-18(16)19;/h4-8,10,15,17,31H,9,11-14H2,1-3H3;1H/t17-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AR-C141990 hydrochloride has no significant activity against MCT-3 (pIC50<5) or MCT-4 (pIC50<5). AR-C141990 hydrochloride inhibits the uptake of [3H]HOCPCA in oocytes expressing MCT1 or 2 in a concentration-dependent manner with IC50s of 0.21 µM and 2.32 µM, respectively.
In Vivo:
AR-C141990 hydrochloride (10 mg/kg; SC) with a parallel decline in plasma concentrations with a half-life around 20 minutes in male NMRI mice (18-22 g) . Application of the corresponding plasma concentrations of AR-C141990 hydrochloride (0.3-90 mg/kg) results in a concentration-dependent decrease in the B/P of HOCPCA with an EC50 of 860 ng/ml. AR-C141990 (100 mg/kg; s.c.) has a moderate prolongation of graft survival for 40 days in PVG rats that received DA cardiac transplants.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.