A1899 (Synonyms: S20951)

Cat. No.: HY-103067 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

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A1899 is a potent and highly selective blocker of the K_2P channel TASK-1. A1899 has IC₅₀ values of 35.1 nM and 7 nM for TASK-1 channels expressed in oocytes and CHO cells, respectively. A1899 is also an I_Kur blocker that can be used for the research of cardiovascular diseases.

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

A1899 Chemical Structure

CAS No. : 498577-46-1

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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500 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

TASK-1

0.035 μM (IC₅₀)

TASK-3

0.318 pg/mL (IC₅₀)

TASK-2

12 μM (IC₅₀)

TASK-4

8.1 μM (IC₅₀)

TREK-1

23.8 μM (pIC₅₀)

TREK-2

8.4 μM (IC₅₀)

TRAAK

>20 μM (IC₅₀)

THIK-1

2.2 μM (IC₅₀)

TRESK

0.9 μM (IC₅₀)

Kv1.1

2.7 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.007 μM Compound: 1; A1899	Inhibition of human TASK1 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay Inhibition of human TASK1 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay	[PMID: 31260312]
CHO	IC₅₀	0.07 μM Compound: 1; A1899	Inhibition of human TASK3 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay Inhibition of human TASK3 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay	[PMID: 31260312]
CHO	IC₅₀	12 μM Compound: 1; A1899	Inhibition of human TASK2 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay Inhibition of human TASK2 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay	[PMID: 31260312]
CHO	IC₅₀	7 nM Compound: 1, A-1899	Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay Inhibition of TASK-1 (unknown origin) expressed in CHO cells by thallium flux assay	[PMID: 25017033]
CHO	IC₅₀	8.1 μM Compound: 1; A1899	Inhibition of human TASK4 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay Inhibition of human TASK4 expressed in CHO cells by Inside-out macro-patches based electrophysiology assay	[PMID: 31260312]

Molecular Weight

500.54

Formula

C₃₀H₂₆F₂N₂O₃

CAS No.

498577-46-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCC1=CC=C(C=C1F)F)C2=CC=CC=C2C3=CC=CC=C3CNC(CC4=CC=C(C=C4)OC)=O

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 : 125 mg/mL (249.73 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	1.9978 mL	9.9892 mL	19.9784 mL
5 mM	0.3996 mL	1.9978 mL	3.9957 mL
10 mM	0.1998 mL	0.9989 mL	1.9978 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

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(per animal)

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(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: 99.72%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (248 KB) HNMR (292 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Streit AK, et al. A specific two-pore domain potassium channel blocker defines the structure of the TASK-1 open pore. J Biol Chem. 2011 Apr 22;286(16):13977-84. [Content Brief]

[2]. Knobloch K, et al. Electrophysiological and antiarrhythmic effects of the novel I(Kur) channel blockers, S9947 and S20951, on left vs. right pig atrium in vivo in comparison with the I(Kr) blockers dofetilide, azimilide, d,l-sotalol and ibutilide. Naunyn Schmiedebergs Arch Pharmacol. 2002 Nov;366(5):482-7. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9978 mL	9.9892 mL	19.9784 mL	49.9461 mL
	5 mM	0.3996 mL	1.9978 mL	3.9957 mL	9.9892 mL
	10 mM	0.1998 mL	0.9989 mL	1.9978 mL	4.9946 mL
	15 mM	0.1332 mL	0.6659 mL	1.3319 mL	3.3297 mL
	20 mM	0.0999 mL	0.4995 mL	0.9989 mL	2.4973 mL
	25 mM	0.0799 mL	0.3996 mL	0.7991 mL	1.9978 mL
	30 mM	0.0666 mL	0.3330 mL	0.6659 mL	1.6649 mL
	40 mM	0.0499 mL	0.2497 mL	0.4995 mL	1.2487 mL
	50 mM	0.0400 mL	0.1998 mL	0.3996 mL	0.9989 mL
	60 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8324 mL
	80 mM	0.0250 mL	0.1249 mL	0.2497 mL	0.6243 mL
	100 mM	0.0200 mL	0.0999 mL	0.1998 mL	0.4995 mL

A1899 Related Classifications

Neurological Disease 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:

A1899498577-46-1S20951A 1899A-1899S 20951S-20951Potassium ChannelKcsATASK-1 channels blockeroocytesCHO cellscardiovascular diseasesI_Kur blockerInhibitorinhibitorinhibit

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A1899 (Synonyms: S20951)

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Complete Stock Solution Preparation Table

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