ChemicalBook--->CAS DataBase List--->118292-41-4

118292-41-4

118292-41-4 Structure

118292-41-4 Structure
IdentificationBack Directory
[Name]

AGN 190299
[CAS]

118292-41-4
[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
[EINECS(EC#)]

604-604-1
[Molecular Formula]

C19H17NO2S
[MDL Number]

MFCD00872121
[MOL File]

118292-41-4.mol
[Molecular Weight]

323.41
Chemical PropertiesBack Directory
[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 DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
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 InformationBack Directory
[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]
.

MaleFemaleMale
Dose (mg kg-1)4.44.40.49
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)
T1/2 (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)
Vβ (L kg-1) --1.14 (0.09)
Vmax (μg min-1) 9.08 (2.89)6.09 (1.22)-
Km (μg mL-1)7.09 (1.35)5.12 (1.19)-
[storage]

Store at -20°C
Spectrum DetailBack Directory
[Spectrum Detail]

AGN 190299(118292-41-4)1HNMR
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