GSK1820795A works as a telmisartan analogue and is an antagonist of hGPR132a. GSK1820795A boiled N-amide is an activator of yeast cells expressing hGPR132a. GSK1820795A is also an angiotensin II antagonist and a partial PPARγ antagonist (compound 38).

Physicochemical Properties

Molecular Formula	C35H34N8
Molecular Weight	566.698066234589
Exact Mass	566.29
CAS #	2650253-86-2
PubChem CID	60165459
Appearance	Off-white to light yellow solid powder
LogP	7.6
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	10
Heavy Atom Count	43
Complexity	865
Defined Atom Stereocenter Count	0
SMILES	N1=C2C(C=C(C3N(CCCC)C4=CC=CC=C4N=3)C=C2)=C(CC2=CC=C(C3=CC=CC=C3C3=NNN=N3)C=C2)N1CCC
InChi Key	XRXMDDDFTLKJHL-UHFFFAOYSA-N
InChi Code	InChI=1S/C35H34N8/c1-3-5-21-42-32-13-9-8-12-31(32)36-35(42)26-18-19-30-29(23-26)33(43(39-30)20-4-2)22-24-14-16-25(17-15-24)27-10-6-7-11-28(27)34-37-40-41-38-34/h6-19,23H,3-5,20-22H2,1-2H3,(H,37,38,40,41)
Chemical Name	5-(1-butylbenzimidazol-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]indazole
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Linoleamide, NPGly, NLGly, and SB-583831 agonists inhibit the response of yeast expressing hGPR132a when GSK1820795A is present [1].
References	[1]. N-Palmitoylglycine and other N-acylamides activate the lipid receptor G2A/GPR132. Pharmacol Res Perspect. 2019;7(6):e00542. [2]. Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists. Bioorg Med Chem Lett. 2014;24(4):1098-1103.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~176.46 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7646 mL	8.8230 mL	17.6460 mL
	5 mM	0.3529 mL	1.7646 mL	3.5292 mL
	10 mM	0.1765 mL	0.8823 mL	1.7646 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.