NGD94-1
Based on 1 Customer Validation
NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research[1][2].
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- Purity: 99.79%
- CAS No.: 178928-68-2
- 화학식: C18H20N6
- 분자량:320.39
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Dopamine Receptor Isoforms
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Biological Activity
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hD4.2 Receptor 3.6 nM (Ki) |
NGD 94-1 shows >600-fold selectivity for the D4.2 receptor over many other targets; however, its selectivity is significantly lower over the 5-HT1A (~50-fold) and 5-HT3 (~200-fold) receptors[2].
NGD 94-1 induces inhibition of cAMP accumulation in HEK293/D4 cells, but does not affect Forskolin (HY-15371)-stimulated cAMP formation in non-transfected HEK293 cells, demonstrating that its inhibitory action is specifically mediated through the transfected dopamine D4 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Young-adult vervet (Cercopithecus aethiops sabaeus) monkeys[1]
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Dosage:1 and 5 mg/kg
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Administration:i.m., 45 min prior to testing
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Result:Significantly reversed the impaired successful performance of PCP-treated subjects (from 58% to 79% accuracy) at 1 mg/kg.
Ameliorated the PCP-induced impairments (from 73% to 86% accuracy) at 5 mg/kg.
Reduced barrier reaching and perseverative responding at both doses in PCP-treated monkeys.
Unaffected response initiation latencies and motor problems in PCP-treated monkeys.
Unaffected accurate performance at 1 mg/kg in saline pretreated monkeys.
Slightly impaired successful performance at 5 mg/kg in saline pretreated monkeys.
Failed to affect response initiation latencies or motor problems at both doses in saline pretreated monkeys.
Failed to affect HVA levels relative to saline in control subjects.
Significantly increased HVA concentrations in the CSF in PCP-treated subjects.
Chemical Information
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CAS No. 178928-68-2
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Appearance Solid
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분자량 320.39
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화학식 C18H20N6
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Color White to off-white
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SMILES
C1(N2CCN(CC3=CN=C(C4=CC=CC=C4)N3)CC2)=NC=CC=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (312.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jentsch JD, et al. Dopamine D4 receptor antagonist reversal of subchronic phencyclidine-induced object retrieval/detour deficits in monkeys. Psychopharmacology (Berl). 1999 Feb;142(1):78-84. [Content Brief]
[2]. Tallman JF, et al. I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Aug;282(2):1011-9. [Content Brief]
[3]. Gazi L, et al. NGD 94-1 as an agonist at human recombinant dopamine D4.4 receptors expressed in HEK293 cells. Eur J Pharmacol. 1999 May 21;372(3):R9-10. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1212 mL | 15.6060 mL | 31.2120 mL | 78.0299 mL |
| 5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | 15.6060 mL | |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL | 7.8030 mL | |
| 15 mM | 0.2081 mL | 1.0404 mL | 2.0808 mL | 5.2020 mL | |
| 20 mM | 0.1561 mL | 0.7803 mL | 1.5606 mL | 3.9015 mL | |
| 25 mM | 0.1248 mL | 0.6242 mL | 1.2485 mL | 3.1212 mL | |
| 30 mM | 0.1040 mL | 0.5202 mL | 1.0404 mL | 2.6010 mL | |
| 40 mM | 0.0780 mL | 0.3901 mL | 0.7803 mL | 1.9507 mL | |
| 50 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5606 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3005 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3901 mL | 0.9754 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL |
NGD94-1 Related Classifications
HY-103405 Related Classifications
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