AR-C141990 hydrochloride

SKU:BHB21900477
Research Validated
Overview
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AR-C141990 hydrochloride (CAS 2250019-94-2) is an inhibitor supplied as a solid. Relevant to Membrane Transporter/Ion Channel research. Molecular formula C26H29ClN4O4S, molecular weight 529.05 g/mol.
Purity 98.2%
CAS Number 2250019-94-2
Molecular Weight 529.05 g/mol
Form Solid
Storage 4°C as supplied; in solvent -80°C
Options selector
Catalog no. Size
HY-119996A-1MG 1 mg
HY-119996A-5MG 5 mg
HY-119996A-10MG 10 mg
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 1 mg, 5 mg, 10 mg
  • Lead time: varies by selected option.
  • Storage: 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: refrigerate at 4°C as soon as possible.
Field Specification
CAS no. 2250019-94-2
Applications
  • Functional Assay (In Vitro)
Molecular weight 529.05
Molecular formula C26H29ClN4O4S
Purity 98.2%
SMILES O=C1N(CC(C)C)C2=C(C(C(N3C[C@H](O)CC3)=O)=C(CC4=CC=NC5=CC=CC=C45)S2)C(N1C)=O.[H]Cl
Form Solid
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-119996A
Main SKU BHB21900477
Inhibitors

Compound Overview

AR-C141990 hydrochloride is a potent inhibitor of lactate transporters (monocarboxylate transporters; MCTs) with pKi values of 7.6 for MCT-1 and 6.6 for MCT-2[1]. It also has immunosuppressive properties and inhibits the graft-versus-host response[2]. It is supplied as a white to off-white solid (C26H29ClN4O4S, MW 529.05) at 98.2% purity.

Physical & Chemical Properties

CAS Number 2250019-94-2
Molecular Formula C26H29ClN4O4S
Molecular Weight 529.05 g/mol
Purity 98.2%
Appearance Solid
Color White to off-white
SMILES O=C1N(CC(C)C)C2=C(C(C(N3C[C@H](O)CC3)=O)=C(CC4=CC=NC5=CC=CC=C45)S2)C(N1C)=O.[H]Cl
Signaling Pathway Membrane Transporter/Ion Channel
Storage 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light).
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

Activity & Target

pKi: 7.6 (MCT-1) and 6.6 (MCT-2)[1]

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Clara Påhlman, et al. Immunosuppressive Properties of a Series of Novel Inhibitors of the Monocarboxylate Transporter MCT-1. Transpl Int. 2013 Jan;26(1):22-9.

[2]. Louise Thiesen, et al. 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. 2015 Aug;354(2):166-74.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.

In Vitro

MCT-3 (pIC50<5) and MCT-4 (pIC50<5) are not significantly affected by AR-C141990 hydrochloride[1]. In oocytes expressing MCT1 or 2, AR-C141990 hydrochloride inhibits the uptake of [3H]HOCPCA in a concentration-dependent manner, with IC50s of 0.21 μM and 2.32 μM, respectively[2].

In Vivo

In male NMRI mice (18-22 g), AR-C141990 hydrochloride (10 mg/kg; SC) shows a parallel decline in plasma concentrations and a half-life of around 20 minutes [2]. Corresponding plasma concentrations of AR-C141990 hydrochloride (0.3-90 mg/kg), when applied, cause the B/P of HOCPCA to decrease in a concentration-dependent way, with an EC50 of 860 ng/ml[2]. In PVG rats that received DA cardiac transplants, AR-C141990 (100 mg/kg; s.c.) moderately prolongs graft survival, for 40 days[1].

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price on some sizes?
A.Availability and lead time for those sizes are confirmed on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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Transcription factor Zhx2 is a checkpoint that programs macrophage polarization and antitumor response. Cell Death Differ 2023 Sep;30(9):2104-2119. PMID: 37582865

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