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Cat. No.: HY-134189

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EST73502

EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.

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CAS No.: 1838622-25-5
화학식: C₁₉H₂₆F₂N₂O₂
분자량:352.42

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

EST73502 Chemical Structure

CAS No.: 1838622-25-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

Ki: 64 nM (MOR), 118 nM (σ1R)^[1]

All Opioid Receptor Isoforms :

All Sigma Receptor Isoforms :

In Vivo

EST73502 (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC₅₀ of 14 mg/kg in the paw pressure test in CD1 male mice^[1].
EST73502 (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice^[1].

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

Animal Model:

Male CD1 mice, PSNL model^[1]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection, twice a day, for 10 days
Result:

Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.

Chemical Information

CAS No. 1838622-25-5
분자량 352.42
화학식 C₁₉H₂₆F₂N₂O₂
SMILES

FC1=CC=C(F)C=C1CCN(CC2)CCC2(O[C@@H]3C)CN(CC)C3=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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)

References

[1]. Mónica García, et al. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain. J Med Chem. 2020 Oct 16. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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상품명:
CAS No.:
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EST73502

All Opioid Receptor Isoforms

All Sigma Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

EST73502 Related Classifications

HY-134189 Related Classifications