PH-064 (tetra(hydrochloride))
Based on 2 publication(s) in Google Scholar
PH-064 tetrahydrochloride (BIM-46187 tetrahydrochloride) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 tetrahydrochloride inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 tetrahydrochloride has potent anti-hyperalgesia activity. PH-064 tetrahydrochloride inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 tetrahydrochloride can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury.
For research use only. We do not sell to patients.
- CAS No.: 2489449-03-6
- Formula: C44H62Cl4N8O2S2
- Molecular Weight:940.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) PH-064 (tetra(hydrochloride))
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Biological Activity
PH-064 (20 μM; 1 h) tetrahydrochloride abrogates the flow-induced dissociation of Gαq/11 from PECAM-1 in HCAECs and attenuates shear stress-induced Akt phosphorylation[2].
PH-064 (10 μM-100 μM; 30 min) tetrahydrochloride concentration-dependently inhibits SERT-mediated 5HT uptake in mouse midbrain and frontal cortex synaptosomes, and also inhibits SERT activity in TRex-SERT cells[3].
PH-064 (for basal IP: even at 10-4 M) tetrahydrochloride has no inhibitory effect on basal IP production in E151A-CCK2R-transfected COS cells, but completely inhibits Gastrin-stimulated IP production (EC50: 34 μM)[5].
PH-064 (10 μM; 1 h) tetrahydrochloride reduces IFNγ generation in RGS2 null BMDMs to the level of WT-BMDMs without affecting BMDM viability[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PH-064 (0.3-3 mg/kg; i.v.) tetrahydrochloride shows dose-dependent anti-hyperalgesic effect in chronic constriction injury (CCI) model in rats[1].
PH-064 (75 mg/kg; p.o.; twice a day; 16 days) tetrahydrochloride exhibits antitumor activity in athymic nude mouse xenografts with E151A-CCK2R-NIH-3T3 cells without apparent toxicity[5].
PH-064 (3 mg/kg; i.v.; 2 h after i.t. LPS) tetrahydrochloride reduces IFNγ expression by 80% in RGS2 null mouse lungs and promotes resolution of lung edema[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats (160-170 g on arrival, allowed to habituate for at least 5 days; Carrageenan-induced hyperalgesia model)[1]
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Dosage:0.1 mg/kg, 1 mg/kg
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Administration:Intravenous injection
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Result:Significantly increased paw withdrawal thresholds (1 mg/kg: 10 g/40 at 0.5 h, 8.9 g/40 at 2.5 h).
Chemical Information
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CAS No. 2489449-03-6
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Molecular Weight 940.96
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Formula C44H62Cl4N8O2S2
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SMILES
O=C([C@H](CSSC[C@@H](C(N1CCN2C([C@@H]1CC3CCCCC3)=NC(C4=CC=CC=C4)=C2)=O)N)N)N([C@H]5CC6CCCCC6)CCN(C5=N7)C=C7C8=CC=CC=C8.Cl.Cl.Cl.Cl
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Synonyms
BIM-46187 tetrahydrochloride
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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.
Publications (2)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Sinapine targeting PLCβ3 EF hands disrupts Gαq-PLCβ3 interaction and ameliorates cardiovascular diseases. [Abstract]2024 Apr:126:155200. PMID: 38387273 -
Biochem Pharmacol
Interplay between G protein-biased and arrestin-biased pathways in 5-HT2AR-mediated ERK activation. [Abstract]2025 Sep:239:117015. PMID: 40473228
Purity & Documentation
References
[1]. Favre-Guilmard C, et al. The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphine. Eur J Pharmacol. 2008 Oct 10;594(1-3):70-6. [Content Brief]
[2]. Dela Paz NG, et al. Rapid flow-induced activation of Gαq/11 is independent of Piezo1 activation. Am J Physiol Cell Physiol. 2019 May 1;316(5):C741-C752. [Content Brief]
[3]. Haase J, et al. Sex and brain region-specific regulation of serotonin transporter activity in synaptosomes in guanine nucleotide-binding protein G(q) alpha knockout mice. J Neurochem. 2021 Oct;159(1):156-171. [Content Brief]
[6]. Joshi JC, et al. RGS2 is an innate immune checkpoint for suppressing Gαq-mediated IFNγ generation and lung injury. iScience. 2025 Jan 27;28(2):111878. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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