Zelnecirnon (Synonyms: RPT193)

Name: Zelnecirnon
Brand: MedChemExpress
SKU: HY-148074
Rating: 4.5 (1 reviews)

Cat. No.: HY-148074 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Zelnecirnon (RPT193) is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. Zelnecirnon can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.

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

Zelnecirnon Chemical Structure

CAS No. : 2366152-15-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 811	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 811	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2050	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3320	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5320	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All CCR Isoform Specific Products:

View All Isoforms

CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CCR4

In Vitro

Zelnecirnon (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC₅₀s of ~370 nM^[2].

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

In Vivo

Zelnecirnon (100 mg/kg; p.o.; once daily; 2 d, 1 d before OVA-challenge) reduces skin inflammation in an acute ovalbumin (OVA)-induced atopic dermatitis model in mice^[2].

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

Animal Model:	Acute ovalbumin (OVA)-induced atopic dermatitis model in mouse^[2]
Dosage:	100 mg/kg
Administration:	Oral gavage; once daily; for 2 days, started 1 day before OVA-challenge (in mouse ear)
Result:	Decreased the ear thickness significantly.

Clinical Trial

Molecular Weight

566.95

Formula

C₂₇H₃₄Cl₃N₅O₂

CAS No.

2366152-15-8

Appearance

Solid

Color

White to off-white

SMILES

C[C@H](C1=C(C=C(C=C1)Cl)Cl)NC2=NC(N3CC([C@@H]4CN([C@H]5C[C@@](C)(C5)C(O)=O)CCC4)C3)=NC(C)=C2Cl

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:

Methanol : 250 mg/mL (440.96 mM; Need ultrasonic)

DMSO : 100 mg/mL (176.38 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	1.7638 mL	8.8191 mL	17.6382 mL
5 mM	0.3528 mL	1.7638 mL	3.5276 mL
10 mM	0.1764 mL	0.8819 mL	1.7638 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.

Molarity Calculator
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:

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (246 KB) HNMR (274 KB) LCMS (263 KB)

Handling Instructions (2659 KB)

References

[1]. Bissonnette R, et al. RPT193, an oral CCR4 inhibitor: Efficacy results from a randomized, placebo-controlled Phase 1b monotherapy trial in patients with moderate-to-severe atopic dermatitis[C]//EXPERIMENTAL DERMATOLOGY. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2021, 30: 40-41.

[2]. Cheng L, et al. Development and first-in-human characterization of a potent oral CCR4 antagonist for the treatment of atopic dermatitis[C]//Journal of Investigative Dermatology. STE 800, 230 PARK AVE, NEW YORK, NY 10169 USA: ELSEVIER SCIENCE INC, 2020, 140(7): S77-S77.

Complete Stock Solution Preparation Table

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

DMSO / Methanol	1 mM	1.7638 mL	8.8191 mL	17.6382 mL	44.0956 mL
	5 mM	0.3528 mL	1.7638 mL	3.5276 mL	8.8191 mL
	10 mM	0.1764 mL	0.8819 mL	1.7638 mL	4.4096 mL
	15 mM	0.1176 mL	0.5879 mL	1.1759 mL	2.9397 mL
	20 mM	0.0882 mL	0.4410 mL	0.8819 mL	2.2048 mL
	25 mM	0.0706 mL	0.3528 mL	0.7055 mL	1.7638 mL
	30 mM	0.0588 mL	0.2940 mL	0.5879 mL	1.4699 mL
	40 mM	0.0441 mL	0.2205 mL	0.4410 mL	1.1024 mL
	50 mM	0.0353 mL	0.1764 mL	0.3528 mL	0.8819 mL
	60 mM	0.0294 mL	0.1470 mL	0.2940 mL	0.7349 mL
	80 mM	0.0220 mL	0.1102 mL	0.2205 mL	0.5512 mL
	100 mM	0.0176 mL	0.0882 mL	0.1764 mL	0.4410 mL

Zelnecirnon Related Classifications

Inflammation/Immunology

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:

Zelnecirnon2366152-15-8RPT193RPT 193RPT-193CCRCC chemokine receptorallergic inflammationatopic dermatitisasthmaTh2orally activeInhibitorinhibitorinhibit

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Zelnecirnon (Synonyms: RPT193)

Customer Review

Zelnecirnon Related Antibodies

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•Related Screening Libraries:

•Related Small Molecules:

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View All CCR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Zelnecirnon Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Zelnecirnon Related Classifications

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