| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SCH 79687 (1.9–13 nM; 30 min) has a high affinity for rat and guinea pig histamine H3 receptors (Ki = 1.9 nM and 13 nM), but has very weak affinity for H1, H2, α2A-adrenergic receptors and imidazoline I2 receptors [1].
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|---|---|
| ln Vivo |
SCH 79687 (0.03-3 mg/kg; intravenous injection; single dose) dose-dependently attenuated the inhibitory effect of (R)-α-methylhistamine on the sympathetic hypertensive response in guinea pigs, with an intravenous ED50 of 0.28 mg/kg [1]. In a feline nasal congestion model induced by compound 48/80, SCH 79687 (3-10 mg/kg; intravenous injection, oral administration; single dose) combined with loratadine exerted a significant decongestant effect via intravenous injection (3 mg/kg) and oral administration (10 mg/kg) without increasing blood pressure [1].
|
| Animal Protocol |
Animal/Disease Models:Hartley (male, anesthetized) [1]
Doses: 0.03 mg/kg; 0.3 mg/kg; 3.0 mg/kg Route of Administration: Intravenous injection; single dose; 5 minutes before (R)-α-methylhistamine administration Experimental Results: The inhibitory effect of (R)-α-methylhistamine-induced sympathetic hypertensive response was attenuated in a dose-dependent manner, with an ED50 of 0.28 mg/kg intravenous injection. At 0.03 mg/kg intravenous injection, the (R)-α-methylhistamine response was inhibited by approximately 10%. At 0.3 mg/kg intravenous injection, the (R)-α-methylhistamine response was inhibited by approximately 65%. At 3.0 mg/kg intravenous injection, the (R)-α-methylhistamine response was inhibited by approximately 80%. Thirty minutes after administration of the ED50 dose (0.28 mg/kg intravenously), the mean plasma concentration reached 25 ng/mL. Animal/Disease Models:(Anesthesia) [1] Doses: 3 mg/kg (intravenous, in combination with loratadine); 10 mg/kg (oral, in combination with loratadine) Route of Administration: Intravenous; single dose; 30 minutes before administration of compound 48/80; oral; single dose; 2 hours before administration of compound 48/80 Experimental Results: Intravenous administration of 3 mg/kg compound 48/80 in combination with loratadine (3 mg/kg intravenous) significantly blocked the increase in nasal resistance caused by compound 48/80 without affecting mean arterial blood pressure. Oral administration of 10 mg/kg in combination with loratadine (10 mg/kg, oral) significantly inhibited the decrease in nasal volume caused by compound 48/80 without affecting systolic blood pressure. When compound 48/80 was used alone, its nasal response was not altered regardless of the dosage. |
| References |
| Molecular Formula |
C18H16CL2N4O
|
|---|---|
| Molecular Weight |
375.25
|
| CAS # |
224585-45-9
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NCC1=CC=C(CC2=CN=CN2)C=C1)NC3=CC(Cl)=CC(Cl)=C3
|
| 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) |
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
|
|---|---|
| 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 | 2.6649 mL | 13.3245 mL | 26.6489 mL | |
| 5 mM | 0.5330 mL | 2.6649 mL | 5.3298 mL | |
| 10 mM | 0.2665 mL | 1.3324 mL | 2.6649 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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