| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
CRF₁ receptor (CRHR1). DMP696 is a selective non-peptidergic CRF1 receptor antagonist.
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| ln Vitro |
DMP696 is a selective CRF1 receptor antagonist that blocks CRF1 receptor-mediated stress signaling. It modulates the HPA axis, which is involved in the stress response. The compound has shown significant efficacy in various animal models for anxiety and depression.
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| ln Vivo |
In mice, DMP696 (3 mg/kg, orally) reduces the consolidation of long-term fear memory, but does not alter its expression or retention. In addition to exhibiting lower synaptosomal GluR1 levels than shock vehicle-treated control mice, WT animals treated with DMP696 for one week beginning 24 hours after foot shock [1]. Little freezing occurred in the rats given varying dosages of DMP696 (1, 3, 10, and 30 mg/kg) throughout the 2-minute shock period. Overall, CREB phosphorylation in the LA and BLA but not in the CeA was significantly reduced in rats treated with DMP696. All time periods saw a decrease in LA and BLA pCREB levels following DMP696 administration; home cage pCREB levels were not substantially different (P>0.05). At each posttreatment period, the pCREB expression levels in the CeA-treated rats, both vehicle- and DMP696-treated rats, were considerably greater than those in their home cages. When compared to animals administered with a vehicle, rats in the 30 ng DMP696 group exhibited noticeably reduced freezing [2].
DMP696 has shown significant efficacy in various animal models. As a selective CRHR1 antagonist, it modulates the HPA axis and blocks CRF1 receptor-mediated stress signaling. The compound is used in neuroscience and pharmacology research for studying anxiety and depression disorders. |
| Enzyme Assay |
In vitro CRF1 receptor binding assays for DMP696 use radioligand binding techniques with membrane preparations from cells expressing recombinant CRF1 receptors. Radiolabeled CRF or selective CRF1 antagonists (such as [¹²⁵I]-sauvagine or [³H]-antalarmin) are used as tracers. Competition binding experiments with varying concentrations of DMP696 determine binding affinity (Ki) and selectivity.
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| Cell Assay |
In vitro cell-based functional assays for DMP696 evaluate its antagonist activity at CRF1 receptors using assays such as cAMP accumulation. Cells expressing recombinant CRF1 receptors are stimulated with CRF to induce cAMP production, and the inhibition of this response by DMP696 is measured. The compound's ability to block CRF-induced signaling confirms its antagonist activity.
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| Animal Protocol |
In vivo animal studies for DMP696 have been conducted in rodent models of anxiety and depression. The compound is administered systemically (typically orally or intraperitoneally), and behavioral endpoints such as elevated plus maze, forced swim test, or tail suspension test are assessed. HPA axis modulation is confirmed by measuring corticosterone levels.
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| ADME/Pharmacokinetics |
DMP696 has a molecular weight of 410.3 g/mol. It is a non-peptidergic compound, suggesting favorable oral bioavailability and blood-brain barrier penetration. Detailed pharmacokinetic parameters such as half-life, Cmax, and oral bioavailability are not extensively reported in the provided literature. The compound is typically formulated for systemic administration.
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| Toxicity/Toxicokinetics |
Specific toxicity data for DMP696 is not extensively reported. As a CRF1 receptor antagonist, its safety profile would need to be established through comprehensive toxicology studies. The compound is classified as a research-grade chemical and is not intended for human use.
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| References |
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| Additional Infomation |
DMP696 (CAS# 202578-52-7) is a selective non-peptidergic CRF1 receptor antagonist. It modulates the HPA axis by blocking CRF₁ receptor-mediated stress signaling. The compound has shown significant efficacy in various animal models for anxiety and depression. It is used in neuroscience and pharmacology research. It has not received FDA approval.
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| Molecular Formula |
C18H21CL2N5O2
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|---|---|
| Molecular Weight |
410.3
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| Exact Mass |
409.107
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| CAS # |
202578-52-7
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| PubChem CID |
9909468
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.634
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| LogP |
3.32
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MDWRPTOUDPFXKK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21Cl2N5O2/c1-10-16(14-6-5-12(19)7-15(14)20)17-21-11(2)22-18(25(17)24-10)23-13(8-26-3)9-27-4/h5-7,13H,8-9H2,1-4H3,(H,21,22,23)
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| Chemical Name |
8-(2,4-dichlorophenyl)-N-(1,3-dimethoxypropan-2-yl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine
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| Synonyms |
DMP-696; DMP 696; DMP696
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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) |
DMSO : ~100 mg/mL (~243.72 mM)
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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 | 2.4372 mL | 12.1862 mL | 24.3724 mL | |
| 5 mM | 0.4874 mL | 2.4372 mL | 4.8745 mL | |
| 10 mM | 0.2437 mL | 1.2186 mL | 2.4372 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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