GSK1820795A

Name: GSK1820795A
Brand: MedChemExpress
SKU: HY-111616
Rating: 4.5 (1 reviews)

Cat. No.: HY-111616 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides. GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38).

For research use only. We do not sell to patients.

GSK1820795A Chemical Structure

CAS No. : 2650253-86-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 636	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 636	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 510	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 820	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 4300	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PPAR Isoform Specific Products:

View All Isoforms

PPARα PPARβ/δ PPARγ PPAR PPARδ

View All Angiotensin Receptor Isoform Specific Products:

View All Isoforms

AT1 Receptor AT2 Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides^[1]. GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38)^[2].

IC₅₀ & Target

AT1 Receptor

0.006 μM (IC₅₀)

hPPARγ

0.25 μM (EC₅₀)

mouse PPARγ

0.27 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.006 μM Compound: 38	Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay	[PMID: 24462665]
CV-1	EC₅₀	> 10 μM Compound: 38	Agonist activity at mouse PPARdelta expressed in CV-1 cells by reporter gene assay Agonist activity at mouse PPARdelta expressed in CV-1 cells by reporter gene assay	[PMID: 24462665]
CV-1	EC₅₀	> 10 μM Compound: 38	Agonist activity at mouse PPARalpha expressed in CV-1 cells by reporter gene assay Agonist activity at mouse PPARalpha expressed in CV-1 cells by reporter gene assay	[PMID: 24462665]
CV-1	EC₅₀	0.25 μM Compound: 38	Partial agonist activity at human PPARgamma expressed in CV-1 cells by reporter gene assay Partial agonist activity at human PPARgamma expressed in CV-1 cells by reporter gene assay	[PMID: 24462665]
CV-1	EC₅₀	0.27 μM Compound: 38	Partial agonist activity at mouse PPARgamma expressed in CV-1 cells by reporter gene assay Partial agonist activity at mouse PPARgamma expressed in CV-1 cells by reporter gene assay	[PMID: 24462665]

In Vitro

GSK1820795A blocks responses of yeast expressing hGPR132a to agonists NPGly, NLGly, linoleamide, and SB-583831^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

566.70

Formula

C₃₅H₃₄N₈

CAS No.

2650253-86-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

CCCN1C(CC2=CC=C(C3=C(C4=NNN=N4)C=CC=C3)C=C2)=C5C(C=CC(C6=NC(C=CC=C7)=C7N6CCCC)=C5)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (176.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (254 KB) HNMR (293 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Foster JR, et al. N-Palmitoylglycine and other N-acylamides activate the lipid receptor G2A/GPR132. Pharmacol Res Perspect. 2019;7(6):e00542. [Content Brief]

[2]. Lamotte Y, Faucher N, Sançon J, et al. Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists. Bioorg Med Chem Lett. 2014;24(4):1098-1103. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7646 mL	8.8230 mL	17.6460 mL	44.1151 mL
	5 mM	0.3529 mL	1.7646 mL	3.5292 mL	8.8230 mL
	10 mM	0.1765 mL	0.8823 mL	1.7646 mL	4.4115 mL
	15 mM	0.1176 mL	0.5882 mL	1.1764 mL	2.9410 mL
	20 mM	0.0882 mL	0.4412 mL	0.8823 mL	2.2058 mL
	25 mM	0.0706 mL	0.3529 mL	0.7058 mL	1.7646 mL
	30 mM	0.0588 mL	0.2941 mL	0.5882 mL	1.4705 mL
	40 mM	0.0441 mL	0.2206 mL	0.4412 mL	1.1029 mL
	50 mM	0.0353 mL	0.1765 mL	0.3529 mL	0.8823 mL
	60 mM	0.0294 mL	0.1471 mL	0.2941 mL	0.7353 mL
	80 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5514 mL
	100 mM	0.0176 mL	0.0882 mL	0.1765 mL	0.4412 mL

GSK1820795A Related Classifications

Cardiovascular Disease Others

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK1820795A2650253-86-2PPARAngiotensin ReceptorPeroxisome proliferator-activated receptorstelmisartananalogselectiveyeastN-acylamidesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

GSK1820795A

Customer Review

GSK1820795A Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PPAR Isoform Specific Products:

View All Angiotensin Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GSK1820795A Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK1820795A Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report