AR-C 141990 hydrochloride

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Description: MCT1 inhibitor
Chemical Name: 5-[[(3R)-3-Hydroxy-1-pyrrolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)-6-(4-quinolinylmethyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for AR-C 141990 hydrochloride

AR-C 141990 hydrochloride is a monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

Technical Data for AR-C 141990 hydrochloride

M. Wt 529.05
Formula C26H28N4O4S.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2250019-94-2
PubChem ID 129316183
InChI Key NFFGLQDNUHBVEY-UNTBIKODSA-N
Smiles O=C(N1C[C@H](O)CC1)C2=C(CC3=C4C(C=CC=C4)=NC=C3)SC(N5CC(C)C)=C2C(N(C)C5=O)=O.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AR-C 141990 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 49.26 100
DMSO 49.26 100

Preparing Stock Solutions for AR-C 141990 hydrochloride

The following data is based on the product molecular weight 529.05. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.89 mL 9.45 mL 18.9 mL
5 mM 0.38 mL 1.89 mL 3.78 mL
10 mM 0.19 mL 0.95 mL 1.89 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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Product Datasheets for AR-C 141990 hydrochloride

Certificate of Analysis / Product Datasheet
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References for AR-C 141990 hydrochloride

References are publications that support the biological activity of the product.

Påhlman et al (2012) Immunosuppressive properties of a series of novel inhibitors of the monocarboxylate transporter MCT-1. Transpl.Int. 26 22 PMID: 23137339

Thiesen et al (2015) In vitro and in vivo evidence for active brain uptake of the GHB analog HOCPCA by the monocarboxylate transporter subtype 1. J.Pharmacol.Exp.Ther. 354 166 PMID: 25986445


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Keywords: AR-C 141990 hydrochloride, AR-C 141990 hydrochloride supplier, AR-C141990, HCl, monocarboxylate, transporter, 1, MCT1, immunosuppressant, graft, versus, host, GvH, transplant, Monocarboxylate, Transporters, 5658, Tocris Bioscience

Citations for AR-C 141990 hydrochloride

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