Takeda103A

Cat. No.: HY-129118 Purity: 98.69%: FAQs
Data Sheet SDS COA Handling Instructions

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Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure.

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

Takeda103A Chemical Structure

CAS No. : 865609-72-9

Size	Price	Stock	Quantity
1 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 337	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	0.02 μM Compound: 1	Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method Inhibition of full length C-terminal hexahistidine tagged GRK2 (unknown origin) S670A mutant expressed in High Five cells using Bac to Bac insect cell expression system using tubulin as substrate by SDS-PAGE method	[PMID: 27050625]

Molecular Weight

463.48

Formula

C₂₄H₂₃F₂N₇O

CAS No.

865609-72-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=C(F)C=CC=C1F)C2=CC=CC(NCC3=NN=C(C4=NC=NC=C4)N3CCC)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (269.70 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	2.1576 mL	10.7880 mL	21.5759 mL
5 mM	0.4315 mL	2.1576 mL	4.3152 mL
10 mM	0.2158 mL	1.0788 mL	2.1576 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.

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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 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.69%

Select Batch:

Data Sheet (268 KB) SDS (251 KB)

COA (247 KB) HNMR (271 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016;59(8):3793-3807. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1576 mL	10.7880 mL	21.5759 mL	53.9398 mL
	5 mM	0.4315 mL	2.1576 mL	4.3152 mL	10.7880 mL
	10 mM	0.2158 mL	1.0788 mL	2.1576 mL	5.3940 mL
	15 mM	0.1438 mL	0.7192 mL	1.4384 mL	3.5960 mL
	20 mM	0.1079 mL	0.5394 mL	1.0788 mL	2.6970 mL
	25 mM	0.0863 mL	0.4315 mL	0.8630 mL	2.1576 mL
	30 mM	0.0719 mL	0.3596 mL	0.7192 mL	1.7980 mL
	40 mM	0.0539 mL	0.2697 mL	0.5394 mL	1.3485 mL
	50 mM	0.0432 mL	0.2158 mL	0.4315 mL	1.0788 mL
	60 mM	0.0360 mL	0.1798 mL	0.3596 mL	0.8990 mL
	80 mM	0.0270 mL	0.1348 mL	0.2697 mL	0.6742 mL
	100 mM	0.0216 mL	0.1079 mL	0.2158 mL	0.5394 mL

Takeda103A Related Classifications

Cardiovascular 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:

Takeda103A865609-72-9OthersGRK2GPCRsheart failureInhibitorinhibitorinhibit

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Takeda103A

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