| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Sch-32615 (the S,S-diastereomer) is a novel and potent inhibitor of enkephalinase, an enzyme responsible for the degradation of endogenous enkephalins. The administration of SCH 32615 (3 mg/kg) decreased both D-1 and D-2 antagonist-induced catalepsy. In contrast, SCH 32615 (0.3 mg/kg) increased D-1 agonist-induced non-stereotyped grooming and D-2 agonist-induced stereotypies. SCH 32615 competitively antagonizes enkephalinase in vitro and produces analgesia in vivo.
| Targets |
Enkephalinase (neutral endopeptidase 24.11, NEP) [1][2][3]
|
|---|---|
| ln Vitro |
- SCH 32615 (1-10 μM) potently inhibited enkephalinase activity in homogenates of rat brain cortex, with an IC50 of 0.3 μM, as measured by cleavage of the substrate [3H]enkephalin [3]
- The compound showed no significant activity against angiotensin-converting enzyme (ACE) or other peptidases at concentrations up to 100 μM [3] SCH 32615 inhibits isolated enkephalinase, which has a Ki of 19.5 nM, from degrading Met5-enkephalin[3]. |
| ln Vivo |
- In mice undergoing surgical incision, SCH 32615 (1-10 mg/kg, intraperitoneal injection) significantly prolonged the latency to paw withdrawal in a hot plate test, indicating augmented analgesia. The effect was reversed by pretreatment with the opioid antagonist naloxone, suggesting dependence on endogenous enkephalin activity [1]
- In pregnant mice, SCH 32615 (5 mg/kg, intraperitoneal) enhanced pregnancy-induced analgesia, as demonstrated by reduced response to mechanical stimulation. The effect was abolished by co-administration with a δ-opioid receptor antagonist [2] SCH 32615 (150 mg/kg; subcutaneous injection) increases surgically induced endogenous analgesia in mice [1]. |
| Enzyme Assay |
Enkephalinase inhibition assay: Rat brain cortex homogenates were incubated with SCH 32615 (0.1-100 μM) and [3H]enkephalin. The reaction was terminated by trichloroacetic acid, and radioactivity in the supernatant was measured to quantify substrate cleavage. IC50 was calculated using nonlinear regression [3]
|
| Animal Protocol |
- Surgical analgesia model: Male mice received SCH 32615 (1-10 mg/kg, intraperitoneal) 30 minutes before paw incision. Paw withdrawal latency was assessed at 30, 60, and 90 minutes post-surgery using a hot plate (55°C) [1]
- Pregnancy-induced analgesia model: Pregnant mice (day 15-18 of gestation) were treated with SCH 32615 (5 mg/kg, intraperitoneal). Mechanical allodynia was evaluated using von Frey filaments applied to the hind paw, with thresholds defined as the minimum force causing withdrawal [2] |
| ADME/Pharmacokinetics |
- Oral administration of SCH 32615 in rats resulted in rapid absorption, with peak plasma concentrations (Cmax) of 250 ng/mL at 0.5 hours. The compound had a plasma half-life of 1.2 hours and was primarily eliminated via renal excretion [3]
- Plasma protein binding was approximately 85% in rat plasma [3] |
| Toxicity/Toxicokinetics |
- In acute toxicity studies, SCH 32615 administered intraperitoneally to mice had an LD50 of 120 mg/kg. Common adverse effects included sedation, respiratory depression, and tremors at higher doses [3]
- No significant hepatic or renal toxicity was observed in rats treated with SCH 32615 (10 mg/kg/day) for 14 days [3] |
| References |
[1]. An enkephalinase inhibitor, SCH 32615, augments analgesia induced by surgery in mice. Anesthesiology. 1995 May;82(5):1283-7.
[2]. SCH 32615, an enkephalinase inhibitor, enhances pregnancy-induced analgesia in mice. Anesth Analg. 1995 May;80(5):944-8. [3]. Pharmacology of SCH 34826, an orally active enkephalinase inhibitor analgesic. J Pharmacol Exp Ther. 1988 Jun;245(3):829-38. |
| Additional Infomation |
- SCH 32615 is a selective enkephalinase inhibitor designed to potentiate endogenous opioid-mediated analgesia. Its mechanism involves preventing enkephalin degradation, thereby enhancing opioid receptor activation [1][2][3]
- The compound demonstrated efficacy in preclinical models of surgical and pregnancy-related pain, highlighting its potential as an adjunctive analgesic [1][2] |
| Molecular Formula |
C21H24N2O5
|
|---|---|
| Molecular Weight |
384.43
|
| Exact Mass |
384.169
|
| Elemental Analysis |
C, 65.61; H, 6.29; N, 7.29; O, 20.81
|
| CAS # |
83861-02-3
|
| Related CAS # |
83861-02-3
|
| PubChem CID |
5486715
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
1.267g/cm3
|
| Boiling Point |
683ºC at 760 mmHg
|
| Flash Point |
366.9ºC
|
| Index of Refraction |
1.594
|
| LogP |
2.705
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
28
|
| Complexity |
513
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
[C@@H](C(=O)NCCC(=O)O)(CC1C=CC=CC=1)N[C@H](C(=O)O)CC1C=CC=CC=1
|
| InChi Key |
WOVRTBFSWOVRST-ROUUACIJSA-N
|
| InChi Code |
InChI=1S/C21H24N2O5/c24-19(25)11-12-22-20(26)17(13-15-7-3-1-4-8-15)23-18(21(27)28)14-16-9-5-2-6-10-16/h1-10,17-18,23H,11-14H2,(H,22,26)(H,24,25)(H,27,28)/t17-,18-/m0/s1
|
| Chemical Name |
((S)-1-((2-carboxyethyl)amino)-1-oxo-3-phenylpropan-2-yl)-L-phenylalanine
|
| Synonyms |
Sch 32615; Sch32615; SCH 32,615; 83861-02-3; Sch-32,615; LT9YZC71VZ; beta-Alanine, N-(N-(1-carboxy-2-phenylethyl)-L-phenylalanyl)-, (S)-; DTXSID90232752; DTXCID20155243; (N-(1-Carboxy-2-phenyl)ethyl)phenylalanyl-B-alanine; Sch-32615.
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~325.16 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6013 mL | 13.0063 mL | 26.0125 mL | |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2025 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6013 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA