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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Tazarotene (AGN190299; trade names Tazorac, Avage, Zorac, and Fabior), a marketed drug, is a third-generation, potent, prescription topical retinoid prodrug used as a cream, gel, or foam for treatment of psoriasis, acne, and sun damaged skin (photodamage).Tazarotene is a member of the acetylenic class of retinoids. Tazarotene is a retinoid prodrug which is converted to its active form, the cognate carboxylic acid of tazarotene (AGN 190299), by rapid deesterification in animals and man. AGN 190299 (“tazarotenic acid”) binds to all three members of the retinoic acid receptor (RAR) RARα, RARβ, and RARγ but shows relative selectivity for RARβ, and RARγ and may modify gene expression. The clinical significance of these findings is unknown.
| ln Vivo |
Analyzing the tazarotenic acid (compound AGN 190299) pharmacokinetic (PK) profile in rats after intravenous dose of AGN 190168 [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) T1/2 (h) 1.64 (0.92) 0.86 (0.14) 0.95 (0.15) V\ (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) -
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| References |
[1]. Chandraratna RA. Tazarotene--first of a new generation of receptor-selective retinoids. Br J Dermatol. 1996;135 Suppl 49:18-25.
[2]. Hsyu PH, et al. Pharmacokinetics of a novel retinoid AGN 190168 and its metabolite AGN 190299 after intravenous administration of AGN 190168 to rats. Biopharm Drug Dispos. 1994;15(5):347-357. [3]. Abramovits W, et al. Treatment of warty dyskeratoma with tazarotenic acid. J Am Acad Dermatol. 2002;46(2 Suppl Case Reports):S4. |
| Additional Infomation |
Tazarotenic acid is 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. It has a role as a keratolytic drug and a teratogenic agent. It is a monocarboxylic acid, a thiochromane, a retinoid and a member of pyridines.
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| Exact Mass |
323.097
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| CAS # |
118292-41-4
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| Related CAS # |
Tazarotenic acid-d6;1794760-38-5
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| PubChem CID |
147525
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| Appearance |
Light yellow to light brown solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
527.5±50.0 °C at 760 mmHg
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| Flash Point |
272.9±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
4.95
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
518
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IQIBKLWBVJPOQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17NO2S/c1-19(2)9-10-23-17-8-4-13(11-16(17)19)3-6-15-7-5-14(12-20-15)18(21)22/h4-5,7-8,11-12H,9-10H2,1-2H3,(H,21,22)
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| Chemical Name |
6-((4,4-dimethylthiochroman-6-yl)ethynyl)nicotinic acid
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| Synonyms |
AGN 190299 AGN-190299 AGN190299 Tazarotenic acid.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~309.21 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02411955 | COMPLETED | Drug: Tazarotene Cream 0.1% Drug: Tazorac® Drug: Placebo |
Acne Vulgaris | Taro Pharmaceuticals USA | 2014-06 | Phase 1 |
| NCT02886702 | COMPLETEDWITH RESULTS | Drug: Tazarotene Cream 0.05% Drug: TAZORAC® (tazarotene) Cream 0.05% Drug: Placebo |
Plaque Psoriasis | Fougera Pharmaceuticals Inc. | 2016-09-19 | Phase 3 |
| NCT02886715 | COMPLETEDWITH RESULTS | Drug: Tazarotene Cream 0.1% Drug: Tazorac® Drug: Placebo |
Acne Vulgaris | Fougera Pharmaceuticals Inc. | 2016-09-21 | Phase 3 |
| NCT00648986 | COMPLETED | Drug: Tazorac | Brittle Nails | Columbia University | 2005-08 | Phase 4 |
| NCT02218034 | COMPLETED | Drug: AGN-190168 Formulation 1 Drug: AGN-190168 Formulation 2 Drug: tazarotene gel 0.1% Drug: tazarotene cream 0.1% |
Acne Vulgaris | Allergan | 2014-08 | Phase 1 |
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