Art. -Nr.: HY-108625

SHA 68

Name: SHA 68
Brand: MedChemExpress
SKU: HY-108625
Price: 103.00 USD
Availability: InStock
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1 Cited Publications

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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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Reinheit: 99.84%
CAS. Nr.: 847553-89-3
Formel: C₂₆H₂₄FN₃O₃
Molecular Weight:445.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SHA 68 Chemical Structure

CAS. Nr.: 847553-89-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 22 nM (Asn¹⁰⁷) and 23.8 nM (Ile¹⁰⁷)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	14 nM Compound: 1b, SHA68	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	[PMID: 24171469]
CHO	IC₅₀	25 nM Compound: 1b, SHA68	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	[PMID: 24171469]
CHO	IC₅₀	420 nM Compound: 1b, SHA68	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	[PMID: 24171469]
CHO	IC₅₀	5.3 nM Compound: 1b, SHA68	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	[PMID: 24171469]

In Vivo

SHA 68 (i.p.; 5 and 50 mg/kg) reduces NPS-induced horizontal activity and vertical rearing and climbing^[1].
SHA 68 (i.v.; 1 mg/kg) has a T_1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a V_ss of 2.53 L/kg^[1].
SHA 68 (i.p.; 2.5 mg/kg) has a T_1/2 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.

Animal Model:

Male C57BL/6 mice age 8-12 weeks^[1]
Dosage:

5 and 50 mg/kg
Administration:

i.p.
Result:

Reduced NPS-induced horizontal activity and vertical rearing and climbing.

Animal Model:

Male C57BL/6 mice age 8-12 weeks^[1]
Dosage:

1 mg/kg (Pharmacokinetic Analysis)
Administration:

i.p.
Result:

Had a T_1/2 of 0.74 hours, a CL of 4.29 mL/min/kg, and a V_ss of 2.53 L/kg.

Chemical Information

CAS. Nr. 847553-89-3
Appearance Solid
Molecular Weight 445.49
Formel C₂₆H₂₄FN₃O₃
Color White to off-white
SMILES

O=C(N1CC2N(C(OC2(C3=CC=CC=C3)C4=CC=CC=C4)=O)CC1)NCC5=CC=C(F)C=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2447 mL

11.2236 mL

22.4472 mL

5 mM

0.4489 mL

2.2447 mL

4.4894 mL

10 mM

0.2245 mL

1.1224 mL

2.2447 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

SHA 68

1 Cited Publications

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SHA 68

ML154

Neuropeptide S (human)

Neuropeptide S (mouse)

CPN-351 TFA

CYM 50769

SHA 68 (Standard)

JNJ-31020028

CART(55-102)(rat)

CART(55-102)(human)

Neuropeptide W-23 (human)

CYM 50769 (Standard)

HT-2157

Publications Citing Use of MedChemExpress (MCE) SHA 68

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

SHA 68

ML154

Neuropeptide S (human)

Neuropeptide S (mouse)

CPN-351 TFA

CYM 50769

SHA 68 (Standard)

JNJ-31020028

CART(55-102)(rat)

CART(55-102)(human)

Neuropeptide W-23 (human)

CYM 50769 (Standard)

HT-2157

Publications Citing Use of MedChemExpress (MCE) SHA 68

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHA 68 Related Classifications

HY-108625 Related Classifications

Bioz