| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
H2 Receptor nNOS 49 μM (IC50)
H2 receptor (histamine H2 receptor) and nNOS (neuronal nitric oxide synthase). |
|---|---|
| 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].
Dimaprit is a selective H2 receptor agonist with less than 0.0001% of the activity of histamine on H1 receptors. It inhibits nNOS with an IC50 of 49 μM. Dimaprit stimulates gastric acid secretion. |
| 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].
In vivo, dimaprit stimulates gastric acid secretion in rats (1.25 μM/kg/min; rapid intravenous injection), cats (2-64 μM/h; intravenous), and dogs (1-100 nM/kg/min; intravenous). It causes dose-dependent falls in blood pressure in cats (0.01-1 μM/kg; intravenous) and vasodilatation in the femoral vascular bed (1-100 nM; intra-arterial injection). It has no effect on heart rate at 1 μM/kg (bolus or intravenous injection). |
| Enzyme Assay |
In vitro receptor binding assays for dimaprit are performed to evaluate its affinity for the H2 receptor. Radioligand binding studies using membrane preparations from cells or tissues expressing the H2 receptor are conducted. The compound's ability to displace a specific radiolabeled H2 ligand is measured to calculate its binding affinity.
|
| Cell Assay |
In vitro cell-based assays are conducted using cells expressing the H2 receptor. The cells are treated with dimaprit, and receptor activation is measured by assessing downstream signaling events such as cAMP accumulation. The compound's selectivity for H2 over H1 is confirmed by testing its activity at both receptors.
|
| Animal Protocol |
In vivo animal studies are conducted in rats, cats, and dogs to evaluate the effects of dimaprit on gastric acid secretion, blood pressure, and vasodilation. The compound is administered via various routes, including intravenous injection and intra-arterial injection.
|
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for dimaprit dihydrochloride. As a research compound, its ADME properties would be characterized in standard preclinical studies.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for dimaprit dihydrochloride. As an H2 receptor agonist, its toxicity profile is expected to be related to its mechanism of action. Standard safety precautions should be followed when handling this compound.
|
| References | |
| Additional Infomation |
Dimaprit is an iminothiocarbamate. It is a histamine H2 receptor agonist, commonly used to study the activity of histamine and its receptor.
Dimaprit dihydrochloride is a selective H2 receptor agonist with less than 0.0001% of the activity of histamine on H1 receptors. It also inhibits nNOS (IC50 = 49 μM). It is used in pharmacological research to study gastric acid secretion, cardiovascular function, and immune regulation. The compound is not approved for human therapeutic use and is strictly for research purposes. |
| Molecular Formula |
C6H17CL2N3S
|
|---|---|
| Molecular Weight |
234.19
|
| Exact Mass |
233.052
|
| CAS # |
23256-33-9
|
| Related CAS # |
23256-33-9 (di-hydrochloride)
|
| PubChem CID |
3077
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.968
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
10
|
| Complexity |
103
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCCSC(=N)N
|
| InChi Key |
OLHQOJYVQUNWPL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C6H15N3S/c1-9(2)4-3-5-10-6(7)8/h3-5H2,1-2H3,(H3,7,8)
|
| Chemical Name |
3-(dimethylamino)propyl carbamimidothioate
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO: 125 mg/mL (533.75 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
