GSK3004774

Name: GSK3004774
Brand: MedChemExpress
SKU: HY-107773
Rating: 4.5 (1 reviews)

Cat. No.: HY-107773 Purity: 98.11%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC₅₀ of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC₅₀ of 50 nM for human CaSR.

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

GSK3004774 Chemical Structure

CAS No. : 2138814-32-9

Size	Price	Stock	Quantity
5 mg	USD 710	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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

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Based on 1 publication(s) in Google Scholar

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	50 nM Compound: 19	Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay Agonist activity at human CaSR expressed in HEK293 cells assessed as increase in intracellular calcium mobilization by fluo-4AM dye based FLIPR assay	[PMID: 28916340]

Molecular Weight

528.69

Formula

C₃₂H₄₀N₄O₃

CAS No.

2138814-32-9

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCCCN1CCC(C(O)=O)CC1)C(C=C2)=CC=C2N(CC3)C[C@H]3N[C@H](C)C4=CC=CC5=C4C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (189.15 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	1.8915 mL	9.4573 mL	18.9147 mL
5 mM	0.3783 mL	1.8915 mL	3.7829 mL
10 mM	0.1891 mL	0.9457 mL	1.8915 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 (sealed storage, away from moisture). 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 (4.73 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 (4.73 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 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 (4.73 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.11%

Select Batch:

Data Sheet (269 KB) SDS (251 KB)

COA (246 KB) HNMR (288 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Sparks SM, et al. Identification of potent, nonabsorbable agonists of the calcium-sensing receptor for GI-specific administration. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4673-4677. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8915 mL	9.4573 mL	18.9147 mL	47.2867 mL
	5 mM	0.3783 mL	1.8915 mL	3.7829 mL	9.4573 mL
	10 mM	0.1891 mL	0.9457 mL	1.8915 mL	4.7287 mL
	15 mM	0.1261 mL	0.6305 mL	1.2610 mL	3.1524 mL
	20 mM	0.0946 mL	0.4729 mL	0.9457 mL	2.3643 mL
	25 mM	0.0757 mL	0.3783 mL	0.7566 mL	1.8915 mL
	30 mM	0.0630 mL	0.3152 mL	0.6305 mL	1.5762 mL
	40 mM	0.0473 mL	0.2364 mL	0.4729 mL	1.1822 mL
	50 mM	0.0378 mL	0.1891 mL	0.3783 mL	0.9457 mL
	60 mM	0.0315 mL	0.1576 mL	0.3152 mL	0.7881 mL
	80 mM	0.0236 mL	0.1182 mL	0.2364 mL	0.5911 mL
	100 mM	0.0189 mL	0.0946 mL	0.1891 mL	0.4729 mL

GSK3004774 Related Classifications

Metabolic Disease

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:

GSK30047742138814-32-9GSK 3004774GSK-3004774CaSRCalcium-sensing receptorInhibitorinhibitorinhibit

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GSK3004774

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GSK3004774 Related Antibodies

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References

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK3004774 Related Classifications

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