5-BDBD

Name: 5-BDBD
Brand: MedChemExpress
SKU: HY-101911
Rating: 5.0 (4 reviews)

Cat. No.: HY-101911 Purity: 99.94%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC₅₀ of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).

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5-BDBD 화학구조

CAS No. : 768404-03-1

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	견적 받기
200 mg	견적 받기

or 대량구매 문의

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

고객리뷰

Based on 4 publication(s) in Google Scholar

Other Forms of 5-BDBD:

5-BDBD (Standard) 견적 받기

4 Publications Citing Use of MCE 5-BDBD

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•Related Screening Libraries:

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View All P2X Receptor Isoform Specific Products:

View All Isoforms

P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

P2X4 Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.5 μM Compound: 5-BDBD	Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as inhibition of ATP-induced calcium influx Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as inhibition of ATP-induced calcium influx	[PMID: 27427902]
CHO	IC₅₀	500 nM Compound: 1; 5-BDBD	Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as reduction in ATP induced calcium influx Antagonist activity at human P2X4 receptor expressed in CHO cells assessed as reduction in ATP induced calcium influx	[PMID: 31746599]
HEK293	IC₅₀	1.2 μM Compound: 5-BDBD	Antagonist activity at human P2X4R transfected in HEK293 cells Antagonist activity at human P2X4R transfected in HEK293 cells	[PMID: 31532206]
HEK293	IC₅₀	9.2 μM Compound: 5-BDBD	Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay	[PMID: 31532206]

In Vitro

5-BDBD inhibits 10 μM ATP-induced currents of rP2X4R-expressing HEK293 cells in a concentration-dependent manner, with an IC₅₀ of 0.75 μM^[1].
? 5-BDBD displaces rightward the ATP concentration-response curve, with an EC₅₀ of 4.7 to 15.9 μM^[1].
? 5-BDBD could be specifically used to discriminate between P2X1R, P2X2aR, P2X2bR, P2X3R, P2X4R, and P2X7R^[1].

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

In Vivo

5-BDBD (28 mg/kg; i.p.; daily for 9 days) can completely blocke the basal hyperalgesia induced by recurrent NTG injection^[2].

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

Animal Model:	Male C57BL/6 mice^[2]
Dosage:	28 mg/kg
Administration:	I.p.; daily for 9 days
Result:	Prevented NTG-induced mechanical hypersensitivity.

분자량

355.19

화학식

C₁₇H₁₁BrN₂O₂

CAS No.

768404-03-1

Appearance

Solid

Color

White to light yellow

SMILES

O=C1CN=C(C2=CC=CC(Br)=C2)C(OC3=CC=CC=C34)=C4N1

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 62.5 mg/mL (175.96 mM; ultrasonic and warming and heat to 60°C; 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	2.8154 mL	14.0770 mL	28.1539 mL
5 mM	0.5631 mL	2.8154 mL	5.6308 mL
10 mM	0.2815 mL	1.4077 mL	2.8154 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.

몰농도 계산기
농도 희석 계산기

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: 15% Solutol HS 15 10% Cremophor EL 35% PEG 400 40% water
Solubility: 9.8 mg/mL (27.59 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 2 mg/mL (5.63 mM); Suspended solution; Need ultrasonic

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.

순도&문서

Purity: 99.94%

Select Batch:

Data Sheet (283 KB) SDS (392 KB)

COA (261 KB) HNMR (135 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Coddou C, et al. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor. Neurosci Lett. 2019;690:219-224. [Content Brief]

[2]. Long T, et al. Microglia P2X4 receptor contributes to central sensitization following recurrent nitroglycerin stimulation. J Neuroinflammation. 2018;15(1):245. Published 2018 Aug 30. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8154 mL	14.0770 mL	28.1539 mL	70.3849 mL
	5 mM	0.5631 mL	2.8154 mL	5.6308 mL	14.0770 mL
	10 mM	0.2815 mL	1.4077 mL	2.8154 mL	7.0385 mL
	15 mM	0.1877 mL	0.9385 mL	1.8769 mL	4.6923 mL
	20 mM	0.1408 mL	0.7038 mL	1.4077 mL	3.5192 mL
	25 mM	0.1126 mL	0.5631 mL	1.1262 mL	2.8154 mL
	30 mM	0.0938 mL	0.4692 mL	0.9385 mL	2.3462 mL
	40 mM	0.0704 mL	0.3519 mL	0.7038 mL	1.7596 mL
	50 mM	0.0563 mL	0.2815 mL	0.5631 mL	1.4077 mL
	60 mM	0.0469 mL	0.2346 mL	0.4692 mL	1.1731 mL
	80 mM	0.0352 mL	0.1760 mL	0.3519 mL	0.8798 mL
	100 mM	0.0282 mL	0.1408 mL	0.2815 mL	0.7038 mL

5-BDBD Related Classifications

Neurological 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:

5-BDBD768404-03-1P2X ReceptorP2XRsselectivecurrentsacutehyperalgesiaNTGATPInhibitorinhibitorinhibit

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5-BDBD

고객리뷰

Other Forms of 5-BDBD:

5-BDBD Related Antibodies

4 Publications Citing Use of MCE 5-BDBD

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All P2X Receptor Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

5-BDBD Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

5-BDBD Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report