Shopping Cart

Your shopping cart is currently empty

SB-705498

Name: SB-705498
Brand: TargetMol
SKU: T6660
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. T6660Cas No. 501951-42-4

SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.

SB-705498

Copy Product Info

😃Good

Purity: 99.81%

Catalog No. T6660Cas No. 501951-42-4

SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$41	In Stock	In Stock
10 mg	$76	In Stock	In Stock
25 mg	$176	In Stock	In Stock
50 mg	$319	In Stock	In Stock
100 mg	$461	In Stock	In Stock
200 mg	$643	-	In Stock
1 mL x 10 mM (in DMSO)	$45	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.81%

Color:White

Resource Download

COA

Product Introduction

Bioactivity

Description	SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.
Targets&IC50	TRPV1 (human):7.1(pIC50), TRPV1 (human):7.6(pKi)
In vitro	SB705498 (0.3 nM-1 μM) effectively blocks capsaicin-induced activation of human TRPV1 channels in 1321N1 and HEK293 cells, with apparent pKi values of 7.5 and 7.6, respectively. A 100 nM SB705498 coapplication rapidly, completely, and reversibly suppresses hTRPV1 in HEK293 cells, without significantly affecting [Ca2+] responses induced by carbachol activation of muscarinic acetylcholine receptors or Ca2+ entry through store-operated channels following thapsigargin-induced Ca2+ store depletion. SB705498 also shows negligible antagonistic effects on TRPV4 activation in HEK293 cells within the 10 pM to 1 μM range and selectively inhibits TRPV1, demonstrating notable potency against rat and guinea pig TRPV1 with pKi values of 7.5 and 7.3, respectively. At 100 nM-10 μM, it rapidly and completely inhibits hTRPV1 in sustained capsaicin responses at -70 mV, with IC50 values of 3 nM and 17 nM at -70 mV and +70 mV, respectively. Furthermore, 1 μM SB705498 fully and reversibly inhibits TRPV1-mediated conductance during the response plateau, uniformly blocking both chemical and physical TRPV1 activation with minimal to no activity against other ion channels, receptors, and enzymes, including inhibition of TRPV1 by heat and altered pH levels.
In vivo	SB705498 demonstrates potent and reversible inhibition of TRPV1 receptor activation through various modes, including vanilloid (capsaicin), heat, and acid mediation. It shows remarkable efficacy at 10 and 30 mg/kg orally, effectively reversing allodynia. Additionally, SB705498 achieves an 80% reduction in allodynia within the guinea pig FCA model at a dosage of 10 mg/kg orally [2].

Chemical Properties

Molecular Weight	429.23
Formula	C₁₇H₁₆BrF₃N₄O
Cas No.	501951-42-4
Smiles	FC(F)(F)c1ccc(nc1)N1CC[C@H](C1)NC(=O)Nc1ccccc1Br
Relative Density.	1.59 g/cm3

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 16 mg/mL (37.28 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (139.79 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (5.82 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3298 mL	11.6488 mL	23.2975 mL	116.4877 mL
5 mM	0.4660 mL	2.3298 mL	4.6595 mL	23.2975 mL
10 mM	0.2330 mL	1.1649 mL	2.3298 mL	11.6488 mL
20 mM	0.1165 mL	0.5824 mL	1.1649 mL	5.8244 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0466 mL	0.2330 mL	0.4660 mL	2.3298 mL
100 mM	0.0233 mL	0.1165 mL	0.2330 mL	1.1649 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc