2489449-03-6
Chemical Structure
PH-064 (tetra(hydrochloride))
Synonym(s): BIM-46187 tetrahydrochloride
- CAS No.: 2489449-03-6
- Formula:C44H62Cl4N8O2S2
- Molecular Weight:940.96
IUPAC Name: (2R,2'R)-3,3'-disulfanediylbis(2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)propan-1-one) tetrahydrochloride
InChIKey: RKTRULIWGAJVGM-FPBFTDTKSA-N
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
Biological Activity: 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[1][2][3][4][5][6].
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PH-064 (tetra(hydrochloride)) | 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. | |||||||||||||||||||||
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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]
- [4]. Auguet M, et al. SYNERGISTIC ANALGESIC INTERACTION BETWEEN MORPHINE AND BIM‐46187. European Journal of Pain, 2006, 10(S1): S89-S89.
- [5]. Silvente-Poirot S, et al. Heterotrimeric G-protein inhibitor BIM-46187 inhibits G-protein coupled receptor dependent tumorigenesis in athymic mice. Cancer Research, 2007, 67(9_Supplement): 5603-5603.
- [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]
