| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
SCH-37370 targets two distinct receptor systems: the platelet-activating factor (PAF) receptor and the histamine H1 receptor. As a dual antagonist, it blocks the binding of both PAF and histamine to their respective receptors. By inhibiting PAF receptor activation, SCH-37370 prevents PAF-induced platelet aggregation and other PAF-mediated inflammatory responses. By blocking histamine H1 receptors, it antagonizes the effects of histamine, which are involved in allergic reactions and inflammation. This dual mechanism of action makes SCH-37370 a potential therapeutic agent for allergic and inflammatory conditions.
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| ln Vitro |
In vitro, SCH-37370 acts as a potent antagonist of both PAF and histamine H1 receptors. It inhibits PAF-induced aggregation of human platelets with an IC50 of 0.6 µM, demonstrating its ability to block PAF-mediated cellular responses. The compound also competes with PAF for binding to specific sites in human lung membrane preparations, with an IC50 of 1.2 mM. Additionally, SCH-37370 blocks [3H]pyrilamine binding to histamine H1 receptors in rat brain membranes. These in vitro studies confirm the compound's dual antagonistic activity at both PAF and histamine receptors.
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| ln Vivo |
In vivo, SCH-37370 has been shown to be orally active. Although specific in vivo efficacy data are limited, its dual antagonism of PAF and histamine suggests potential therapeutic applications in allergic and inflammatory conditions such as asthma, allergic rhinitis, and other PAF-mediated disorders. The compound's oral bioavailability makes it suitable for systemic administration. Further in vivo studies would be required to fully characterize its efficacy and safety in disease models.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assays for SCH-37370 include radioligand binding assays for both PAF and histamine H1 receptors. For the PAF receptor, the compound's ability to displace a labeled PAF ligand from human lung membrane preparations is measured. For the histamine H1 receptor, the compound's ability to displace [3H]pyrilamine from rat brain membranes is assessed. These assays provide quantitative measures of the compound's binding affinity (IC50) at both targets. The assays confirm the dual antagonistic activity of SCH-37370.
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| Cell Assay |
In vitro cellular assays for SCH-37370 include platelet aggregation assays using human platelets. Platelets are pre-incubated with varying concentrations of SCH-37370, and aggregation is induced with PAF. The extent of aggregation is measured using a platelet aggregometer, and the IC50 for inhibition of aggregation is determined. The compound's ability to inhibit histamine-induced responses can also be assessed in appropriate cell lines expressing H1 receptors, such as measuring intracellular calcium mobilization or other downstream signaling events.
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| Animal Protocol |
In vivo animal experiments for SCH-37370 are not extensively documented. However, as a dual PAF and histamine antagonist, the compound could be evaluated in animal models of asthma, allergic rhinitis, or other inflammatory conditions. Standard protocols would involve oral or intraperitoneal administration of SCH-37370 to rodents, followed by challenge with PAF or histamine to assess the compound's ability to inhibit the resulting physiological responses. Endpoints may include bronchoconstriction, vascular permeability, or inflammatory cell infiltration.
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| ADME/Pharmacokinetics |
SCH-37370 has a molecular weight of 352.86 g/mol and a molecular formula of C21H21ClN2O. The compound is orally active. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability are not extensively reported in the available literature. However, the compound's oral activity suggests adequate systemic absorption. SCH-37370 is soluble in DMSO and other organic solvents, and its formulation for in vivo studies typically involves standard vehicles for oral or parenteral administration.
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| Toxicity/Toxicokinetics |
SCH-37370 has been evaluated as an impurity in the synthesis of desloratadine. No significant toxicity has been reported in the available literature. However, as a dual PAF and histamine antagonist, the compound's safety profile would need to be comprehensively evaluated in toxicology studies. Potential adverse effects may include those associated with H1 receptor antagonism, such as sedation or anticholinergic effects, although these are typically less pronounced with newer antihistamines.
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| References | |
| Additional Infomation |
SCH-37370 is a potent, orally active dual antagonist of platelet-activating factor (PAF) and histamine. It is also known as N-Acetyldesloratadine and is an impurity in the synthesis of desloratadine. The compound inhibits PAF-induced platelet aggregation and blocks histamine H1 receptor binding. SCH-37370 is a research compound with potential applications in allergic and inflammatory diseases. It is not an approved drug and requires further development to establish its therapeutic utility.
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| Molecular Formula |
C21H21CLN2O
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|---|---|
| Molecular Weight |
352.862
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| Exact Mass |
352.134
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| CAS # |
117796-52-8
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| PubChem CID |
60680
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| Appearance |
White to off-white solid powder
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| Density |
1.257g/cm3
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| Boiling Point |
546.9ºC at 760mmHg
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| Flash Point |
284.5ºC
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| Vapour Pressure |
5.15E-12mmHg at 25°C
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| Index of Refraction |
1.626
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| LogP |
4.215
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
25
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC2CCC3=CC=CN=C3/C(=C3/CCN(C(=O)C)CC/3)/C=2C=C1
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| InChi Key |
FLTBEMVEAFMWDD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21ClN2O/c1-14(25)24-11-8-15(9-12-24)20-19-7-6-18(22)13-17(19)5-4-16-3-2-10-23-21(16)20/h2-3,6-7,10,13H,4-5,8-9,11-12H2,1H3
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| Chemical Name |
1-[4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]ethanone
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| Synonyms |
SCH37370; SCH 37370; SCH-37370
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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 | 2.8340 mL | 14.1699 mL | 28.3399 mL | |
| 5 mM | 0.5668 mL | 2.8340 mL | 5.6680 mL | |
| 10 mM | 0.2834 mL | 1.4170 mL | 2.8340 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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