SHA 68
Based on 1 publication(s) in Google Scholar
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn107 and NPSR Ile107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
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- Purity: 99.84%
- CAS No.: 847553-89-3
- 화학식: C26H24FN3O3
- 분자량:445.49
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
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CART(55-102)(human) -
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CYM 50769 (Standard) -
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Publications Citing Use of MedChemExpress (MCE) SHA 68
More
Biological Activity
제품 설명
IC50 & Target
IC50: 22 nM (Asn107) and 23.8 nM (Ile107)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
14 nM
Compound: 1b, SHA68
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Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced ERK activation after 20 mins by HTRF assay
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[PMID: 24171469] |
| CHO | IC50 |
25 nM
Compound: 1b, SHA68
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Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting
Displacement of [125I]Tyr10-NPS from human neuropeptide S receptor expressed in CHO cells after 1.5 hrs by liquid scintillation counting
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[PMID: 24171469] |
| CHO | IC50 |
420 nM
Compound: 1b, SHA68
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Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as inhibition of NPS-induced calcium mobilization after 10 mins by fluorescence assay
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[PMID: 24171469] |
| CHO | IC50 |
5.3 nM
Compound: 1b, SHA68
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Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay
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[PMID: 24171469] |
In Vivo
SHA 68 (i.v.; 1 mg/kg) has a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg[1].
SHA 68 (i.p.; 2.5 mg/kg) has a T1/2 of 0.43 hours, a CL of 4.56 mL/min/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice age 8-12 weeks[1]
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Dosage:5 and 50 mg/kg
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Administration:i.p.
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Result:Reduced NPS-induced horizontal activity and vertical rearing and climbing.
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Animal Model:Male C57BL/6 mice age 8-12 weeks[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis)
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Administration:i.p.
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Result:Had a T1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a Vss of 2.53 L/kg.
Chemical Information
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CAS No. 847553-89-3
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Appearance Solid
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분자량 445.49
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화학식 C26H24FN3O3
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Color White to off-white
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SMILES
O=C(N1CC2N(C(OC2(C3=CC=CC=C3)C4=CC=CC=C4)=O)CC1)NCC5=CC=C(F)C=C5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Peptides
Neuropeptide S promotes maintenance of newly formed dendritic spines and performance improvement after motor learning in mice. [Abstract]2022 Oct:156:170860. PMID: 35970276
용액&용해도
In Vitro:
DMSO : 100 mg/mL (224.47 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
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 (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Okamura N, et al. Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor.J Pharmacol Exp Ther. 2008 Jun;325(3):893-901. [Content Brief]
[2]. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2447 mL | 11.2236 mL | 22.4472 mL | 56.1180 mL |
| 5 mM | 0.4489 mL | 2.2447 mL | 4.4894 mL | 11.2236 mL | |
| 10 mM | 0.2245 mL | 1.1224 mL | 2.2447 mL | 5.6118 mL | |
| 15 mM | 0.1496 mL | 0.7482 mL | 1.4965 mL | 3.7412 mL | |
| 20 mM | 0.1122 mL | 0.5612 mL | 1.1224 mL | 2.8059 mL | |
| 25 mM | 0.0898 mL | 0.4489 mL | 0.8979 mL | 2.2447 mL | |
| 30 mM | 0.0748 mL | 0.3741 mL | 0.7482 mL | 1.8706 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4029 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1224 mL | |
| 60 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9353 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7015 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5612 mL |
SHA 68 Related Classifications
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