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  3. Cenerimod

Cenerimod (Synonyms: ACT-334441)

Cat. No.: HY-17606 Purity: ≥98.0%
Handling Instructions

Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.

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

Cenerimod Chemical Structure

Cenerimod Chemical Structure

CAS No. : 1262414-04-9

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 85 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 85 In-stock
Estimated Time of Arrival: December 31
10 mg USD 145 In-stock
Estimated Time of Arrival: December 31
25 mg USD 249 In-stock
Estimated Time of Arrival: December 31
50 mg USD 435 In-stock
Estimated Time of Arrival: December 31
100 mg USD 739 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous[1][2].

IC50 & Target

S1PR1

1 nM (EC50)

S1PR5

36 nM (EC50)

S1PR5

228 nM (EC50)

S1PR4

2134 nM (EC50)

In Vitro

Cenerimod is a highly potent S1P1 receptor agonists in (35S)-GTPγS assays using HUVEC cell membrane preparations, with an EC50 of 2 nM[1].
Cenerimod activates G protein and increases Ca2+ signaling in CHO cells, with EC50s of 1 nM and 124 nM, respectively[1].
Cenerimod (5 μM; 24 h) inhibits collagen production in fibroblasts[2].

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

In Vivo

Cenerimod (0.1-10 mg/kg; a single p.o.) reversibly reduces the number of circulating lymphocytes in a dose‐dependent manner in rats[1].
Cenerimod (6 mg/kg/day for 30 days; p.o.) attenuates disease in a mouse experimental autoimmune encephalitis (EAE) model[1].
Cenerimod (10 mg/kg/day for 42 days; p.o.) attenuates skin and lung fibrosis in Scl-cGVHD mice[2].

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

Animal Model: Male Wistar rats weighing 294-510 g[1]
Dosage: 0.1, 0.3, 1, 3 and 10 mg/kg
Administration: A single p.o.
Result: Effectively and reversibly reduced the blood lymphocyte counts, with a plateau reached after a single oral dose of 1 mg/kg.
Clinical Trial
Molecular Weight

453.53

Formula

C₂₅H₃₁N₃O₅

CAS No.
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 : ≥ 100 mg/mL (220.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2049 mL 11.0246 mL 22.0493 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 mL
10 mM 0.2205 mL 1.1025 mL 2.2049 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
Cenerimod
Cat. No.:
HY-17606
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