| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H29ClN4O4S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
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.
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.
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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