Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
EP4 2.35 nM (Ki) EP4 3 nM (IC50)
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ln Vitro |
The rat EP4 receptor's Ki is 1.11 nM, while the rat EP4 receptor's cAMP levels and rat EP4 receptor's CREB activation have EC50 values of 2.66 nM and 0.17 nM, respectively. KMN-80 is tested for both EP4 receptor binding and rat EP2 and EP4 receptor activation[1]. On day nine, the ALP enzyme activity is measured and BMCs, which are isolated from young female rats, are treated once during plating with different doses of KMN-80. ALP EC50 values for KMN-80 (0-100 nM) exhibit significant differences from those corresponding to PGE2 and PGE1, with EC50 values of 82.1 nM and 29.3 nM, respectively, for the activation of ALP enzyme activity in young female rat BMCs, old female rat BMCs, and young male rat BMCs[1]. In EP4-transfected HEK293 cells, KMN-80 has been demonstrated to increase secreted alkaline phosphatase gene reporter activity with an EC50 value of 0.19 nM, exhibiting >5,000 and 50,000-fold selectivity against EP2 and TP, respectively[2]. While the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells, KMN-80 can induce the differentiation of bone marrow stem cells from both young and old rats into osteoblasts in vitro (EC50s=20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM[2]. With Ki values of 880 nM and 2.349 nM for hEP3 and hEP4, respectively, KMN-80 binds to human EP receptor subtypes[2].
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References |
[1]. M Li, et al. Prostaglandin E(2) Receptors in Bone Formation. Int Orthop
[2]. Thomas A Owen, et al. KMN-159, a Novel EP 4 Receptor Selective Agonist, Stimulates Osteoblastic Differentiation in Cultured Whole Rat Bone Marrow. Gene. 2020 Jul 20;748:144668. |
Molecular Formula |
C21H33NO4
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Molecular Weight |
363.49
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CAS # |
1628759-75-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1CC[C@H](/C=C/[C@H]([C@@H](C)CC#CCC)O)N1CCCCCCC(=O)O
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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 | 2.7511 mL | 13.7555 mL | 27.5111 mL | |
5 mM | 0.5502 mL | 2.7511 mL | 5.5022 mL | |
10 mM | 0.2751 mL | 1.3756 mL | 2.7511 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.