ChemicalBook CAS DataBase List 118292-41-4

118292-41-4

Name	AGN 190299
CAS	118292-41-4
EINECS(EC#)	604-604-1
Molecular Formula	C19H17NO2S
MDL Number	MFCD00872121
Molecular Weight	323.41
MOL File	118292-41-4.mol

Synonyms

CS-2016 AGN 190299 Tazarotene Acid Tazarotenic acid Tazarotenic acid (AGN 190299) Tazarotenic Acid (10mM in DMSO) Tazarotene Impurity 1（Tazarotenic Acid） 4-Dimethylthiochroman-6-yl)ethynyl)nicotinic acid 6-(4,4-Dimethyl-thiochroman-7-ylethynyl)-nicotinic acid 6-(2-(4,4-Dimethylthiochroman-6-yl)ethynyl)nicotinic acid 6-[[(3,4-Dihydro-4,4-dimethyl-2H-1-benzothiopyran)-6-yl]ethynyl]nicotinic acid 6-[(4,4-diMethyl-3,4-dihydro-2H-thiochroMen-6-yl)ethynyl]pyridine-3-carboxylic acid TAZAROTENIC ACID; 118292-41-4; 6-(2-(4;4-DIMETHYLTHIOCHROMAN-6-YL)ETHYNYL)NICOTINIC ACID 6-((3,4-Dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl)-3-pyridinecarboxylic acid 3-Pyridinecarboxylic acid, 6-((3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl)- 6-[2-(3,4-Dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl]-3-pyridine carboxylic acid 3-Pyridinecarboxylicacid, 6-[2-(3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl]- Tazarotenic Acid 13C2,D2Q: What is Tazarotenic Acid 13C2,D2 Q: What is the CAS Number of Tazarotenic Acid 13C2,D2 Q: What are the applications of Tazarotenic Acid 13C2,D2

Chemical Properties

Melting point	>190°C (dec.)
Boiling point	527.5±50.0 °C(Predicted)
density	1.31
storage temp.	-20°C Freezer
solubility	DMSO (Slightly, Sonicated), Methanol (Slightly, Sonicated)
form	Solid
pka	3.30±0.10(Predicted)
color	Pale Yellow to Brown

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H315-H319-H335
Precautionary statements	P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

Hazard Information

Chemical Properties

Pale Yellow Solid

Uses

Tazarotenic acid is the major active metabolite

Uses

Tazarotenic acid is the major active metabolite of Tazarotene (T010050).

Uses

The principle active metabolite

Definition

ChEBI: A thiochromane that is acetylene in which the hydrogens are replaced by 5-carboxypyridin-2-yl and 4,4-dimethylthiochroman-6-yl groups. It is the active form of the prodrug tazarotene.

Biological Activity

Tazarotene is transformed to tazarotenic acid with the help of esterases. Tazarotenic acid regulates the pathogenic aspects of psoriasis through normalizing abnormal keratinocyte differentiation. It possesses strong anti-hyperproliferative effects in skin and reduces inflammation.''Tazarotenic acidan active metabolite of tazaroteneis a potent and selective agonist of the retinoid receptor (RAR) th at binds to RARαRARβand RARγ. Tazarotenic acid relatively selective activates RARβ and RARγ. Tazarotenic acid is a first xenobiotic substrate of human retinoic acid hydroxylase CYP26A1 and CYP26B1.

in vivo

Assessment of Pharmacokinetics (PK) profile of Tazarotenic acid (Compound AGN 190299) after an intravenous of AGN 190168 in rats^[1]
.

	Male	Female	Male
Dose (mg kg^-1)	4.4	4.4	0.49
AUC (μg h mL^-1)	9.31 (2.14)	9.78 (1.36)	0.594 (0.95)
CL (mL min^-1 kg^-1)	7.96 (1.59)	7.62 (0.85)	14.0 (2.2)
k (h^-1)	0.562 (0.339)	0.820 (0.146)	0.741 (0.115)
T_1/2 (h)	1.64 (0.92)	0.86 (0.14)	0.95 (0.16)
V₀ (L kg^-1)	0.43 (0.05)	0.49 (0.06)	1.31 (1.15)
V_β (L kg^-1)	-	-	1.14 (0.09)
V_max (μg min^-1)	9.08 (2.89)	6.09 (1.22)	-
K_m (μg mL^-1)	7.09 (1.35)	5.12 (1.19)	-

storage

Store at -20°C

Spectrum Detail

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