| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
H2 Receptor nNOS 49 μM (IC50)
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|---|---|
| ln Vitro |
Less than 0.0001% of histamine's action on H1-receptors is present in dimaprit[1]. With a 49±14 μM IC50, dimaprit (0.1 nM-100 μM) inhibits nNOS concentration in a concentration-dependent manner[2].
|
| ln Vivo |
Cats (2-64 μM/h; IV), dogs (1-100 nM/kg/min; IV), and rats (1.25 μM/kg/min; rapid IV injection) all exhibit increased stomach acid output in response to dimaprit[1]. (0.01-1 μM/kg; intravenously every 5 minutes) results in dose-dependent drops in cats' blood pressure. Dimaprit (1 μM/kg; bolus or intravenous injection) has no effect on heart rate, but it produces vasodilatation in the femoral vascular bed when administered intraarterially (1–100 nM)[1].
|
| References |
[1]. Parsons ME, et, al. Dimaprit -(S-[3-(N,N-dimethylamino)prophyl]isothiourea) - a highly specific histamine H2 -receptor agonist. Part 1. Pharmacology. Agents Actions. 1977 Mar; 7(1): 31-7.
[2]. Paquay JB, et, al. Nitric oxide synthase inhibition by dimaprit and dimaprit analogues. Br J Pharmacol. 1999 May; 127(2): 331-4. |
| Molecular Formula |
C6H17CL2N3S
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|---|---|
| Molecular Weight |
234.19
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| CAS # |
23256-33-9
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| SMILES |
CN(C)CCCSC(=N)N.Cl.Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 125 mg/mL (533.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.88 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 (8.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2700 mL | 21.3502 mL | 42.7004 mL | |
| 5 mM | 0.8540 mL | 4.2700 mL | 8.5401 mL | |
| 10 mM | 0.4270 mL | 2.1350 mL | 4.2700 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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