GSK417651A

Chemical compound

GSK417651A
Identifiers

IUPAC name 3,4-dihydro-1H-isoquinolin-2-yl-[2-(4-methoxyanilino)-1,3-thiazol-4-yl]methanone
CAS Number	736945-96-3^Y
PubChem CID	1096735
UNII	WV82DEG4YA
CompTox Dashboard (EPA)	DTXSID701336625
Chemical and physical data
Formula	C₂₀H₁₉N₃O₂S
Molar mass	365.45 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES COC1=CC=C(C=C1)NC2=NC(=CS2)C(=O)N3CCC4=CC=CC=C4C3
InChI InChI=1S/C20H19N3O2S/c1-25-17-8-6-16(7-9-17)21-20-22-18(13-26-20)19(24)23-11-10-14-4-2-3-5-15(14)12-23/h2-9,13H,10-12H2,1H3,(H,21,22) Key:NTXBDULODNTCKP-UHFFFAOYSA-N

GSK417651A is a chemical compound which acts as a blocker of the TRPC family of calcium channels, with selectivity for the TRPC3 and TRPC6 subtypes. It has been used to investigate the role of TRPC3/6 channels in heart function.^[1]^[2]^[3]

References

^ Xu X, Lozinskaya I, Costell M, Lin Z, Ball JA, Bernard R, Behm DJ, Marino JP, Schnackenberg (2013). "CG Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists". Biophysical Journal. 104 (2): 454a. Bibcode:2013BpJ...104..454X. doi:10.1016/j.bpj.2012.11.2513.
^ Wen H, Gwathmey JK, Xie LH (2020). "Role of Transient Receptor Potential Canonical Channels in Heart Physiology and Pathophysiology". Frontiers in Cardiovascular Medicine. 7: 24. doi:10.3389/fcvm.2020.00024. PMC 7052113. PMID 32158769.
^ Al-Shammari H, Latif N, Sarathchandra P, McCormack A, Rog-Zielinska EA, Raja S, et al. (2020). "Expression and function of mechanosensitive ion channels in human valve interstitial cells". PLOS ONE. 15 (10): e0240532. Bibcode:2020PLoSO..1540532A. doi:10.1371/journal.pone.0240532. PMC 7561104. PMID 33057457.

TRP channel modulators

TRPA

Activators	4-Hydroxynonenal 4-Oxo-2-nonenal 4,5-EET 12S-HpETE 15-Deoxy-Δ^12,14-prostaglandin J2 α-Sanshool (ginger, Sichuan and melegueta peppers) Acrolein Allicin (garlic) Allyl isothiocyanate (mustard, radish, horseradish, wasabi) AM404 ASP-7663 Bradykinin Cannabichromene (cannabis) Cannabidiol (cannabis) Cannabigerol (cannabis) Cinnamaldehyde (cinnamon) CR gas (dibenzoxazepine; DBO) CS gas (2-chlorobenzal malononitrile) Cuminaldehyde (cumin) Curcumin (turmeric) Dehydroligustilide (celery) Diallyl disulfide Dicentrine (Lindera spp.) Farnesyl thiosalicylic acid Formalin Gingerols (ginger) Hepoxilin A3 Hepoxilin B3 Hydrogen peroxide Icilin Isothiocyanate JT-010 Ligustilide (celery, Angelica acutiloba) Linalool (Sichuan pepper, thyme) Methylglyoxal Methyl salicylate (wintergreen) N-Methylmaleimide Nicotine (tobacco) Oleocanthal (olive oil) Paclitaxel (Pacific yew) Paracetamol (acetaminophen) PF-4840154 Phenacyl chloride Polygodial (Dorrigo pepper) Shogaols (ginger, Sichuan and melegueta peppers) Tear gases Tetrahydrocannabinol (cannabis) Tetrahydrocannabiorcol Thiopropanal S-oxide (onion) Umbellulone (Umbellularia californica) WIN 55,212-2
Blockers	A-967079 AM-0902 Dehydroligustilide (celery) HC-030031 Nicotine (tobacco) PF-04745637 Ruthenium red

Activators

4-Hydroxynonenal
4-Oxo-2-nonenal
4,5-EET
12S-HpETE
15-Deoxy-Δ^12,14-prostaglandin J2
α-Sanshool (ginger, Sichuan and melegueta peppers)
Acrolein
Allicin (garlic)
Allyl isothiocyanate (mustard, radish, horseradish, wasabi)
AM404
ASP-7663
Bradykinin
Cannabichromene (cannabis)
Cannabidiol (cannabis)
Cannabigerol (cannabis)
Cinnamaldehyde (cinnamon)
CR gas (dibenzoxazepine; DBO)
CS gas (2-chlorobenzal malononitrile)
Cuminaldehyde (cumin)
Curcumin (turmeric)
Dehydroligustilide (celery)
Diallyl disulfide
Dicentrine (Lindera spp.)
Farnesyl thiosalicylic acid
Formalin
Gingerols (ginger)
Hepoxilin A3
Hepoxilin B3
Hydrogen peroxide
Icilin
Isothiocyanate
JT-010
Ligustilide (celery, Angelica acutiloba)
Linalool (Sichuan pepper, thyme)
Methylglyoxal
Methyl salicylate (wintergreen)
N-Methylmaleimide
Nicotine (tobacco)
Oleocanthal (olive oil)
Paclitaxel (Pacific yew)
Paracetamol (acetaminophen)
PF-4840154
Phenacyl chloride
Polygodial (Dorrigo pepper)
Shogaols (ginger, Sichuan and melegueta peppers)
Tear gases
Tetrahydrocannabinol (cannabis)
Tetrahydrocannabiorcol
Thiopropanal S-oxide (onion)
Umbellulone (Umbellularia californica)
WIN 55,212-2

Blockers

TRPC

Activators	Adhyperforin (St John's wort) Diacyl glycerol GSK1702934A Hyperforin (St John's wort) Substance P
Blockers	DCDPC DHEA-S Flufenamic acid GSK417651A GSK2293017A Meclofenamic acid N-(p-Amylcinnamoyl)anthranilic acid Niflumic acid Pregnenolone sulfate Progesterone Pyr3 Tolfenamic acid

TRPM

Activators	ADP-ribose BCTC Calcium (intracellular) CIM-0216 Cold Coolact P Cooling Agent 10 Eucalyptol (eucalyptus) Frescolat MGA Frescolat ML Geraniol Hydroxycitronellal Icilin Linalool Menthol (mint) PMD 38 Pregnenolone sulfate Rutamarin (Ruta graveolens) Steviol glycosides (e.g., stevioside) (Stevia rebaudiana) Sweet tastants (e.g., glucose, fructose, sucrose; indirectly) Thio-BCTC WS-12
Blockers	AMG-333 Capsazepine Clotrimazole DCDPC Elismetrep Flufenamic acid Meclofenamic acid Mefenamic acid N-(p-Amylcinnamoyl)anthranilic acid Nicotine (tobacco) Niflumic acid Ononetin PF-05105679 RQ-00203078 Ruthenium red Rutamarin (Ruta graveolens) Tolfenamic acid TPPO TRPM4-IN-5

Activators

ADP-ribose
BCTC
Calcium (intracellular)
CIM-0216
Cold
Coolact P
Cooling Agent 10
Eucalyptol (eucalyptus)
Frescolat MGA
Frescolat ML
Geraniol
Hydroxycitronellal
Icilin
Linalool
Menthol (mint)
PMD 38
Pregnenolone sulfate
Rutamarin (Ruta graveolens)
Steviol glycosides (e.g., stevioside) (Stevia rebaudiana)
Sweet tastants (e.g., glucose, fructose, sucrose; indirectly)
Thio-BCTC
WS-12

Blockers

TRPML

Activators	EVP21 MK6-83 ML-SA1 ML2-SA1 PI(3,5)P₂ SF-22 SN-2
Blockers	ML-SI3 PI(4,5)P₂

TRPP

Activators	Triptolide (Tripterygium wilfordii)
Blockers	Ruthenium red

TRPV

Activators	2-APB 5',6'-EET 9-HODE 9-oxoODE 12S-HETE 12S-HpETE 13-HODE 13-oxoODE 20-HETE α-Sanshool (ginger, Sichuan and melegueta peppers) Allicin (garlic) AM404 Anandamide Bisandrographolide (Andrographis paniculata) Camphor (camphor laurel, rosemary, camphorweed, African blue basil, camphor basil) Cannabidiol (cannabis) Cannabidivarin (cannabis) Capsaicin (chili pepper) Carvacrol (oregano, thyme, pepperwort, wild bergamot, others) DHEA Diacyl glycerol Dihydrocapsaicin (chili pepper) Estradiol Eugenol (basil, clove) Evodiamine (Euodia ruticarpa) Gingerols (ginger) GSK1016790A Heat Hepoxilin A3 Hepoxilin B3 Homocapsaicin (chili pepper) Homodihydrocapsaicin (chili pepper) Incensole (incense) Lysophosphatidic acid Low pH (acidic conditions) Menthol (mint) N-Arachidonoyl dopamine N-Oleoyldopamine N-Oleoylethanolamide Nonivamide (PAVA) (PAVA spray) Nordihydrocapsaicin (chili pepper) Paclitaxel (Pacific yew) Paracetamol (acetaminophen) Phenylacetylrinvanil Phorbol esters (e.g., 4α-PDD) Piperine (black pepper, long pepper) Polygodial (Dorrigo pepper) Probenecid Protons RhTx Rutamarin (Ruta graveolens) Resiniferatoxin (RTX) (Euphorbia resinifera/pooissonii) Shogaols (ginger, Sichuan and melegueta peppers) Tetrahydrocannabivarin (cannabis) Thymol (thyme, oregano) Tinyatoxin (Euphorbia resinifera/pooissonii) Tramadol Vanillin (vanilla) Zucapsaicin
Blockers	α-Spinasterol (Vernonia tweediana) AMG-517 AMG-9810 Asivatrep BCTC Cannabigerol (cannabis) Cannabigerolic acid (cannabis) Cannabigerovarin (cannabis) Cannabinol (cannabis) Capsazepine DCDPC DHEA DHEA-S Flufenamic acid GRC-6211 HC-067047 Lanthanum Mavatrep Meclofenamic acid N-(p-Amylcinnamoyl)anthranilic acid NGD-8243 Niflumic acid Pregnenolone sulfate RN-1734 RN-9893 Ruthenium red SB-366791 SB-705498 Tivanisiran Tolfenamic acid TRPV3-74a

Activators