AR-C 141990 hydrochloride

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Cat.No. 5658 - AR-C 141990 hydrochloride | C26H28N4O4S.HCl
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
Literature

Biological Activity

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

M. Wt 529.05
Formula C26H28N4O4S.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 529.05. Batch specific molecular weights may vary from batch to batch due to solvent 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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