| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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Purity: ≥98%
CAY10471 (rotation +) (also known as TM-30089) is a novel, potent and highly selective prostaglandin D2 receptor CRTH2 antagonist with a Ki of 0.6 nM for hCRTH2, it is selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2. CAY10471 Racemate (Compound 13) inhibits PGD2-induced inositol phosphate or cAMP formation, suppresses β-arrestin translocation with IC50s of 12 and 3 nM, respectivel
| ln Vitro |
In PC12 cells, 15dPGJ2-induced p38 MAP kinase phosphorylation is greatly reduced by CAY10471 (1 μM; 1-24 hours) [1].
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| ln Vivo |
In chronic contact hypersensitivity (CHS) and IgE-CAI models, CAY10471 (oral therapy; 2 mg/kg; challenge day 22 or more than 10 consecutive days) showed decreased inflammation. While it greatly reduces inflammation in mice, it only partially blocks CRTH2 [2]. When compared to the vehicle, CAY10471 (oral treatment; 20 mg/kg; twice daily; beginning 3/4/5 days before to UUO) dramatically reduced cortical interstitial collagen deposition (8.40% vs. 14.85%). When compared to vehicle, oral treatment of UUO after three days likewise significantly reduced cortical interstitial collagen deposition (9.63% vs. 14.44%). On cortical interstitial collagen deposition, however, oral treatment beginning five days after UUO had no effect in comparison to vehicle (14.61% vs. 15.09%). UUO stands for unilateral ureteral obstruction [3].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: PC12 Cell Tested Concentrations: 1 μM Incubation Duration: 1 or 24 hrs (hours) Experimental Results: Blocks 15d-PGJ2-induced p38 MAP kinase activation. |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse, DP−/− mice, CRTH2−/− mice[2]
Doses: 2 mg/kg Route of Administration: po (po (oral gavage)) one time/day; on the 22nd day or for more than 10 days Challenge Experimental Results: Dramatically inhibited CHS and IgE-CAI inflammatory respons. Animal/Disease Models: C57BL/6 mice [3] Doses: 20 mg/kg Route of Administration: po (po (oral gavage)) twice (two times) daily; start 3/4/5 days before UUO Experimental Results: Slows the progression of renal fibrosis in obstructed kidneys. |
| References |
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| Molecular Formula |
C21H21FN2O4S
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|---|---|
| Molecular Weight |
416.46600
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| Exact Mass |
416.12
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| CAS # |
627865-18-3
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| Related CAS # |
CAY10471 Racemate;844639-57-2
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| PubChem CID |
11384493
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
654.7±65.0 °C at 760 mmHg
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| Flash Point |
349.7±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.664
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| LogP |
4.09
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
704
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1CCC2=C(C1)C3=CC=CC=C3N2CC(=O)O)S(=O)(=O)C4=CC=C(C=C4)F
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| InChi Key |
CANCTKXGRVNXFP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-15)17-4-2-3-5-19(17)24(20)13-21(25)26/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)
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| Chemical Name |
(+)-3-[[(4-fluorophenyl)sulfonyl]methylamino]-1,2,3,4-tetrahydro-9H-carbazole-9-acetic acid
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| Synonyms |
CAY-10471 CAY 10471 CAY10471 TM30089 TM-30089 TM 30089
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4011 mL | 12.0057 mL | 24.0113 mL | |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8023 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4011 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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