1206123-97-8 | Etrasimod Arginine
CAS:1206123-97-8
MF:C32H40F3N5O5
MW:631.7
EINECS:
MDL No.:
Properties
Appearance white to beige powder
storage temp. -10 to -25°C
Application:
Etrasimod Arginine is an orally effective S1P receptor modulator that primarily acts on the S1P1 receptor and exhibits partial agonistic activity towards the S1P4 receptor. It can alleviate inflammation in a mouse colitis model with CD4+CD45RBhighT cell metastasis.
| Category | Details |
|---|---|
| Specific Applications |
1. Moderate-to-Severe Active Ulcerative Colitis: induces/maintains clinical remission by sequestering lymphocytes in lymph nodes to reduce intestinal inflammation. 2. Investigational Applications: Crohn's disease (Phase III), atopic dermatitis (Phase II/III), eosinophilic esophagitis (Phase II), alopecia areata (early clinical trials); leverages S1P1/4/5 receptor modulation for immune regulation. 3. Pharmaceutical Formulation: Active pharmaceutical ingredient (API) for oral tablet production; arginine salt form enhances water solubility, dissolution rate, and oral bioavailability vs. etrasimod free base. |
| Key Synthetic Intermediates (Chemical Name, CAS No., Role) |
1. Etrasimod Free Acid (Etrasimod, CAS 1206123-37-6): acidic precursor; reacts with L-arginine to form the arginine salt (API). 2. L-Arginine (CAS 74-79-3): Basic amino acid; forms a 1:1 salt with etrasimod free acid to improve solubility and formulation compatibility. 3. (R)-Ethyl 2-(7-((4-cyclopentyl-3-(trifluoromethyl)benzyl)oxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetate (CAS 1206123-96-7): Chiral ester intermediate; hydrolyzed to etrasimod free acid. 4. Ethyl 2-(7-((4-cyclopentyl-3-(trifluoromethyl)benzyl)oxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetate (CAS 1206124-13-1): Precursor to the chiral ester; undergoes resolution/ asymmetric synthesis to form the (R)-enantiomer. 5. 4-(Chloromethyl)-1-cyclopentyl-2-(trifluoromethyl)benzene (CAS 957208-65-0): Aromatic alkylating agent; forms the benzyl ether linkage in the etrasimodN structure. |
Synonyms:
Etrasimod arginine
APD334 L-Arginine
1206123-97-8
Velsipity
L-arginine mono((3R)-7-((4-cyclopentyl-3-(trifluoromethyl)phenyl)methoxy)-1,2,3,4-tetrahydrocyclopenta(b)indol-3-yl)acetate
L-Arginine, (3R)-7-((4-cyclopentyl-3-(trifluoromethyl)phenyl)methoxy)-1,2,3,4-tetrahydrocyclopent(b)indole-3-acetate (1:1)
Velsipity
APD334 arginine
etrasimod L-arginine
APD 334 L-arginine
Etrasimod arginine
(2S)-2-amino-5-(diaminomethylideneamino)pentanoic acid;2-[(3R)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
(R)-2-(7-((4-Cyclopentyl-3-(trifluoromethyl)benzyl)oxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (S)-2-amino-5-guanidinopentanoic acid(1:1)
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