| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AZD3676 (1 pM-100 nM (5-HT1A); 0.01 nM-1 μM (5-HT1B); 16 h, room temperature) showed nanomolar affinity for the 5-HT1A (Ki = 0.13 nM) and 5-HT1B (Ki = 2.4 nM) receptors in cynomolgus monkey brain homogenate[1]. AZD3676 (0.4-20 μM; ~1 μM (predicted Cmax)) showed concentration-dependent plasma protein binding, with free fractions ranging from 0.014 (human) to 0.37 (guinea pig) in different species at the predicted maximum therapeutic concentration of ~1 μM[1].
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| ln Vivo |
AZD3676 (10 μmol/kg; subcutaneous injection; single dose) significantly reversed R-8-OH-DPAT-induced cognitive impairment in C57BL/6 mice, as evidenced by the recovery of frozen behavior in the situational fear conditioned reflex test [1]. AZD3676 (1-10 μmol/kg; subcutaneous injection, oral administration; single dose) significantly reversed scopolamine-induced cognitive impairment in C57BL/6 mice, as evidenced by the recovery of frozen behavior in the situational fear conditioned reflex test [1]. AZD3676 (0.03-3 μmol/kg; subcutaneous injection; single dose) dose-dependently occupied 5-HT1ₐ receptors in healthy C57BL/6 mice, with a half-maximal receptor occupancy rate of 0.05 μmol/kg (subcutaneous injection) in the prefrontal cortex [1]. AZD3676 (0.1–10 μmol/kg; subcutaneous injection; single dose) occupies 5-HT1A receptors in healthy Sprague Dawley rats in a dose-dependent manner, with a half-maximal occupancy of 0.17 μmol/kg subcutaneous injection in the prefrontal cortex [1]. AZD3676 (0.3–10 μmol/kg; subcutaneous injection; single dose) occupies 5-HT1A and 5-HT1B receptors in healthy Dunkin Hartley guinea pigs in a dose-dependent manner, with half-maximal occupancy of 0.3 μmol/kg and 1.2 μmol/kg subcutaneous injection, respectively [1]. AZD3676 (0.16–0.82 μmol/kg; intravenous injection; initial low-dose bolus followed by maintenance infusion) occupies 5-HT1A receptors in healthy cynomolgus monkeys in a dose-dependent manner, with a plasma Ki value of 84 nM achieving half-maximal occupancy in the prefrontal cortex [1]. AZD3676 (0.1-1.8 μmol/kg; intravenous injection; initial low-dose bolus followed by maintenance infusion) dose-dependently occupied 5-HT1B receptors in healthy cynomolgus monkeys, with a plasma Ki value of 72 nM in the occipital cortex to achieve a maximum half-maximum occupancy [1].
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| Animal Protocol |
Animal/Disease Models:C57BL/6[1]
Doses: 10 μmol/kg Route of Administration: Subcutaneous injection; single dose Experimental Results: Significantly reversed R-8-OH-DPAT-induced memory deficits, manifested as increased freezing behavior compared to mice treated with R-8-OH-DPAT alone. Animal/Disease Models:C57BL/6[1] Doses: 3 μmol/kg; 10 μmol/kg; 1 μmol/kg Route of Administration: Subcutaneous injection; Single dose; Oral administration; Single dose Experimental Results: Subcutaneous injection of 3 μmol/kg, subcutaneous injection of 10 μmol/kg and oral administration of 1 μmol/kg significantly reversed scopolamine-induced memory deficits, manifested as increased freezing behavior compared to mice treated with scopolamine alone. Animal/Disease Models:C57BL/6[1] Doses: 0.03 μmol/kg; 0.1 μmol/kg; 0.3 μmol/kg; 1 μmol/kg; 3 μmol/kg Route of Administration: Subcutaneous injection; Single dose Experimental Results: Subcutaneous injection dose occupied the 5-HT1ₐ receptor in the frontal lobe of mice in a dose-dependent manner, with a half maximum receptor occupancy rate of 0.05 μmol/kg. Animal/Disease Models:Sprague Dawley[1] Doses: 0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg; 10 μmol/kg Route of Administration: Subcutaneous injection; Single dose Experimental Experimental Results: Subcutaneous injection dose occupied the 5-HT1ₐ receptor in the subcutaneous frontal lobe of rats in a dose-dependent manner, with a half maximum receptor occupancy rate of 0.17 μmol/kg. |
| References |
| Molecular Formula |
C22H26N4O2
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|---|---|
| Molecular Weight |
378.48
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| CAS # |
1259929-13-9
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C=1OC2=C(C=CC=C2N3CCN(CCC4=NC=CC=C4)CC3)C1)N(C)C
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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 | 2.6421 mL | 13.2107 mL | 26.4215 mL | |
| 5 mM | 0.5284 mL | 2.6421 mL | 5.2843 mL | |
| 10 mM | 0.2642 mL | 1.3211 mL | 2.6421 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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