2. GPCR/G Protein
  3. Adenosine Receptor
  4. MIPS521

MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.

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MIPS521 Chemical Structure

MIPS521 Chemical Structure

CAS No. : 1146188-19-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 42 In-stock
5 mg USD 90 In-stock
10 mg USD 140 In-stock
50 mg USD 420 In-stock
100 mg USD 650 In-stock
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Based on 1 publication(s) in Google Scholar

MIPS521 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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  • Purity & Documentation

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Description

MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine[1][2].

IC50 & Target[1]

A1AR

 

In Vitro

MIPS521 (compound 13o) (3-10 μM) improves the ability of R-PIA to promote A1AR-mediated ERK1/2 phosphorylation[1].
MIPS521 (0.3-30 μM; pretreament for 10 min, co-treatment for 30 min) produces a concentration-dependent potentiation of signalling by ADO in an inhibition of cAMP assay (expressed as a percentage of the inhibition of 3 μM forskolin-mediated cAMP) in CHO cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MIPS521 Related Antibodies
In Vivo

MIPS521 (1-30 μg in 10 μL; intrathecal administration) reverses mechanical hyperalgesia in rats, promoting robust antinociception[2].
MIPS521 (10 μg in 10 μL; intrathecal administration) significantly reduces spontaneous pain in a conditioned place preference model[2].
MIPS521 (1-30 μg in 10 μL; intrathecal administration) reduces eEPSCs in spinal cord from nerve-injured rats, with a pEC50 of 6.9. The maximum MIPS521-induced decrease in synaptic current amplitude is significantly greater in nerve-injured rats than in sham surgery controls[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female Sprague-Dawley rats (7-12 weeks) were performed a partial nerve ligation (PNL) or sham surgery[2]
Dosage: 1, 3, 10, 30 μg in 10 μL
Administration: Intrathecal administration
Result: Reduced eEPSCs in spinal cord from nerve-injured rats and reversed mechanical hyperalgesia.
Molecular Weight

449.80

Formula

C19H10ClF6NOS
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(C1=C(N)SC=C1C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C3=CC=C(C=C3)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.58 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2232 mL 11.1161 mL 22.2321 mL
5 mM 0.4446 mL 2.2232 mL 4.4464 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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. 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 2.2232 mL 11.1161 mL 22.2321 mL 55.5803 mL
5 mM 0.4446 mL 2.2232 mL 4.4464 mL 11.1161 mL
10 mM 0.2223 mL 1.1116 mL 2.2232 mL 5.5580 mL
15 mM 0.1482 mL 0.7411 mL 1.4821 mL 3.7054 mL
20 mM 0.1112 mL 0.5558 mL 1.1116 mL 2.7790 mL
25 mM 0.0889 mL 0.4446 mL 0.8893 mL 2.2232 mL
30 mM 0.0741 mL 0.3705 mL 0.7411 mL 1.8527 mL
40 mM 0.0556 mL 0.2779 mL 0.5558 mL 1.3895 mL
50 mM 0.0445 mL 0.2223 mL 0.4446 mL 1.1116 mL
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MIPS521 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MIPS5211146188-19-3MIPS 521MIPS-521Adenosine ReceptorP1 receptorA1ARpainInhibitorinhibitorinhibit

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