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Chemical Structure| 545395-94-6 Chemical Structure| 545395-94-6

Structure of AMG9810
CAS No.: 545395-94-6

Chemical Structure| 545395-94-6

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AMG9810 is an antagonist of TRPV1 receptor with IC50 of 17 nM and exhibits antihyperalgesic properties in rat model.

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Product Details of AMG9810

CAS No. :545395-94-6
Formula : C21H23NO3
M.W : 337.41
SMILES Code : O=C(NC1=CC=C(OCCO2)C2=C1)/C=C/C3=CC=C(C(C)(C)C)C=C3
MDL No. :MFCD00955103
InChI Key :GZTFUVZVLYUPRG-IZZDOVSWSA-N
Pubchem ID :680502

Safety of AMG9810

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H319-H413
Precautionary Statements:P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CHO-TRPV1 cells 1 μM HXA3 induced intracellular Ca2+ accumulation Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6721-6
CHO cells 5 μM block proton-induced TRPV1 activation to study ASIC3 currents Acta Pharmacol Sin. 2020 Aug;41(8):1049-1057
HEK293T cells 10 μM To evaluate the effect of AMG9810 on recombinant Ca v3 channels, results showed that AMG9810 at 10 μM had no effect on Ca v3-mediated currents. Br J Pharmacol. 2019 Jul;176(13):2264-2278
BV-2 cells 1 μM 1 hour AMG9810 significantly reduced the enhancing effect of CBD on phagocytosis in BV-2 cells, but to a lesser extent than other antagonists. Br J Pharmacol. 2014 May;171(9):2426-39
Carotid body type I cells 10 µM To block TRPV1 receptors and investigate their role in LPA-induced carotid body responses. The results showed that AMG9810 could block the increase in carotid body nerve activity caused by LPA Nat Commun. 2018 Oct 2;9(1):4030
rat sensory neurons 1 μM HXA3 significantly increased free Ca2+ levels, an effect attenuated by 61% with the TRPV1-selective antagonist AMG9810 (1 μM) Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6721-6
rat dorsal root ganglia (DRG) neurons 5 μM block proton-induced TRPV1 activation to study ASIC currents Acta Pharmacol Sin. 2020 Aug;41(8):1049-1057
CHO-TRPV1 cells 100, 300, 1000 nM AMG9810 antagonized capsaicin-mediated contractions in a competitive manner Br J Pharmacol. 2012 Mar;165(6):1801-1812

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male Sprague-Dawley rats Monosodium iodoacetate (MIA)-induced osteoarthritis model Intraperitoneal injection 30 mg/kg Single dose AMG9810 effectively blocked thermal hypersensitivity, but failed to block high dose MIA-induced weight asymmetry or ongoing pain Pain. 2012 Apr;153(4):924-933
NSG mice Xenograft model of systemic MM with BM involvement Intraperitoneal (i.p.) injections 10 mg/kg Twice per week, for a total of 6 injections Bortezomib/AMG9810 treatment effectively reduced tumor burden in the BM of MM-bearing mice J Hematol Oncol. 2020 Nov 25;13(1):158
Rats Carrageenan-induced inflammatory hyperalgesia model Intrathecal injection 10 μg Single dose, 30 min pretreatment AMG9810 significantly attenuated carrageenan-evoked tactile allodynia and thermal hyperalgesia Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6721-6
Rats Cisplatin-induced neuropathic pain model Intraperitoneal injection 3 mg/kg Single administration To evaluate the impact of TRPV1 antagonist AMG9810 on the anti-allodynic effects of endocannabinoid modulators. Results showed that AMG9810 completely blocked the anti-allodynic efficacy of FAAH inhibitors (URB597 and URB937) but not the MGL inhibitor (JZL184). Pharmacol Res. 2013 Jan;67(1):94-109

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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