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RS-102895 Hydrochloride CCR antagonist

Name: RS-102895 Hydrochloride
Brand: Selleck Chemicals
SKU: S7538
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S7538

RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.

Chemical Structure

Molecular Weight: 426.86

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Quality Control

Batch: S753801 DMSO]85 mg/mL]false]Ethanol]85 mg/mL]false]Water]Insoluble]false Purity: 99.88%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.88

Related Targets	K-Ras CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras
Other CCR Products	Cenicriviroc Vicriviroc Malate Adaptavir (DAPTA) ZK756326 2HCl SB-297006 INCB3344 RS102895 Vicriviroc maleate AZD2098 R243

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (10.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	426.86	Formula	C₂₁H₂₂ClF₃N₂O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1173022-16-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RS-102895 HCl			Smiles	Cl.FC(F)(F)C1=CC=C(CCN2CCC3(CC2)OC(=O)NC4=CC=CC=C34)C=C1

Mechanism of Action

Targets/IC₅₀/Ki	human α1a receptor (Cell-free assay) 130 nM human α1d receptor (Cell-free assay) 320 nM CCR2 (Cell-free assay) 360 nM 5-HT1a receptor (Cell-free assay) 470 nM
In vitro	An in vitro chemotaxis assay validates the effect of RS-102895 on leukocyte chemotaxis toward CCL2. The results suggest that increased CCL2 in SS kidneys is important in the early recruitment of leukocytes, and blockade of this recruitment by administering RS-102895 subsequently blunts the renal damage and hypertension.<sup><a class="sref" href="#s_ref">[2]</a></sup>
In vivo	The functional role of the CCL2/CCR2 pathway is tested by daily administration of CCR2 antagonist RS-102895. Blood pressure, renal leukocyte infiltration, and renal damage are evaluated. The results demonstrates that RS-102895 treatment ameliorates renal damage and hypertension after 21 days of high-salt diet. It is determined that renal leukocyte infiltration is blunted by day 3 of the high-salt diet.<sup><a class="sref" href="#s_ref">[2]</a></sup>
References	[1] https://pubmed.ncbi.nlm.nih.gov/10770925/ [2] https://pubmed.ncbi.nlm.nih.gov/32150444/

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