Ro 0437626
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM).
For research use only. We do not sell to patients.
- CAS No.: 134362-79-1
- Formula: C27H35N5O4S
- Molecular Weight:525.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All P2X Receptor Isoforms
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Biological Activity
Description
IC50 & Target
IC50: 3 μM (P2X1 receptor)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
>100 μM
Compound: 1
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Inhibitory concentration against human P2X purinoceptor 3 (hP2X3) expressed in CHO-K1 cells
Inhibitory concentration against human P2X purinoceptor 3 (hP2X3) expressed in CHO-K1 cells
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[PMID: 15927468] |
| CHO-K1 | IC50 |
3 μM
Compound: 1
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Inhibitory concentration against human P2X purinoceptor 1 (hP2X1) expressed in CHO-K1 cells
Inhibitory concentration against human P2X purinoceptor 1 (hP2X1) expressed in CHO-K1 cells
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[PMID: 15927468] |
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female rat (urethane-anaesthetized)[3]
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Dosage:1 and 10 μmol/kg
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Administration:I.v.
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Result:Caused a reduction in postinfusion isovolumetric contractions.
Chemical Information
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CAS No. 134362-79-1
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Molecular Weight 525.66
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Formula C27H35N5O4S
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SMILES
O=C(C1=NC2=CC=CC=C2N1)N[C@H](CC3=CSC=N3)C(N[C@@H](CC4CCCCC4)[C@@H](O)[C@H](C5CC5)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295. [Content Brief]
[2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613. [Content Brief]
[3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)