| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
SC-51322 targets the prostaglandin E2 (PGE2) receptor subtype EP1. It is a selective antagonist of this receptor. The EP1 receptor is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. By selectively binding to and blocking the EP1 receptor, SC-51322 inhibits PGE2-mediated signaling.
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| ln Vitro |
SC-51322 is a highly potent EP1 receptor antagonist with a Ki of 13.8 nM. It also has a pA2 of 8.1, indicating high affinity. It is a selective antagonist, and its activity is confirmed through binding and functional assays. Its analgesic properties have been demonstrated in vivo.
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| ln Vivo |
SC-51322 displays analgesic properties in vivo. This suggests that it is effective in animal models of pain, likely through its antagonism of the EP1 receptor. Its ability to block PGE2-mediated pain signaling makes it a valuable tool for studying pain mechanisms and as a potential therapeutic for pain management.
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| Enzyme Assay |
The in vitro activity of SC-51322 is assessed using radioligand binding assays. The compound is tested for its ability to displace a labeled ligand from the EP1 receptor. The Ki value of 13.8 nM is determined from these assays. Its selectivity is confirmed by testing against other prostanoid receptors.
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| Cell Assay |
The antagonist activity of SC-51322 can be assessed in functional cell-based assays. For example, its ability to block PGE2-induced calcium mobilization or other downstream signaling events can be measured in cells expressing the EP1 receptor. The pA2 value of 8.1 is derived from such functional assays.
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| Animal Protocol |
While specific in vivo protocols are not detailed, SC-51322 has been shown to have analgesic properties in vivo. This suggests it has been evaluated in animal models of pain, such as the formalin test or the acetic acid-induced writhing test. In these models, the compound would be administered, and its ability to reduce pain-related behaviors would be measured.
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| ADME/Pharmacokinetics |
SC-51322 has a molecular weight and formula that are not detailed in the provided excerpts. It is a potent and selective EP1 receptor antagonist with a Ki of 13.8 nM. It is a valuable research tool for studying EP1 receptor signaling. It is typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
SC-51322 is a research compound, and its toxicity profile is not detailed in the provided sources. In animal studies, it was administered at doses that produced analgesic effects, suggesting it was tolerated. However, comprehensive toxicology studies would be required for its development as a therapeutic agent.
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| References | |
| Additional Infomation |
SC-51322 (CAS#: 146032-79-3) is a potent and selective antagonist of the prostaglandin E2 (PGE2) receptor subtype EP1. It has a Ki of 13.8 nM and a pA2 of 8.1. SC-51322 displays analgesic properties in vivo and is a valuable research tool for studying EP1 receptor signaling in pain, arthritis, and neurodegenerative diseases.
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| Molecular Formula |
C22H25CLN3O4S
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|---|---|
| Molecular Weight |
462.97
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| Exact Mass |
457.086
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| CAS # |
146032-79-3
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| PubChem CID |
9933831
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| Appearance |
White to off-white solid powder
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| LogP |
5.956
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
628
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CQBVTZDISUKDSX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20ClN3O4S/c23-16-7-8-20-18(12-16)26(13-15-4-1-2-6-19(15)30-20)22(28)25-24-21(27)9-11-31-14-17-5-3-10-29-17/h1-8,10,12H,9,11,13-14H2,(H,24,27)(H,25,28)
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| Chemical Name |
3-chloro-N'-[3-(furan-2-ylmethylsulfanyl)propanoyl]-6H-benzo[b][1,4]benzoxazepine-5-carbohydrazide
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| Synonyms |
SC51322; SC 51322; SC-51322
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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 (~218.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1600 mL | 10.7998 mL | 21.5997 mL | |
| 5 mM | 0.4320 mL | 2.1600 mL | 4.3199 mL | |
| 10 mM | 0.2160 mL | 1.0800 mL | 2.1600 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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