AM-0902

Name: AM-0902
Brand: MedChemExpress
SKU: HY-108329
Rating: 4.5 (0 reviews)

Cat. No.: HY-108329 Purity: 99.73%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC₅₀s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.

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AM-0902 화학구조

CAS No. : 1883711-97-4

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

Other Forms of AM-0902:

AM-0902 (Standard) 견적 받기

Featured Recommendations

•Related Screening Libraries:

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View All TRP Channel Isoform Specific Products:

View All Isoforms

TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC₅₀s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.

IC₅₀ & Target

IC50: 71 nM (rTRPA1), 131 nM (hTRPA1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	> 40 μM Compound: 27; AM-0902	Agonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay Agonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay	[PMID: 26942860]
CHO	EC₅₀	> 40 μM Compound: 27; AM-0902	Agonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay Agonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells by 45Ca2+ uptake assay	[PMID: 26942860]
CHO	IC₅₀	0.01 μM Compound: 27; AM-0902	Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of hypo osmolarity buffer-induced 45Ca2+ uptake preincubated for 10 mins followed by hypo osmolarity buffer addition measured after 3 mins by TopCount microplate scintillator counting method Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of hypo osmolarity buffer-induced 45Ca2+ uptake preincubated for 10 mins followed by hypo osmolarity buffer addition measured after 3 mins by TopCount microplate scintillator counting method	[PMID: 26942860]
CHO	IC₅₀	0.019 μM Compound: 27; AM-0902	Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of methylglyoxal-induced 45Ca2+ uptake preincubated for 10 mins followed by methylglyoxal addition measured after 3 mins by TopCount microplate scintillator counting method Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of methylglyoxal-induced 45Ca2+ uptake preincubated for 10 mins followed by methylglyoxal addition measured after 3 mins by TopCount microplate scintillator counting method	[PMID: 26942860]
CHO	IC₅₀	0.02 μM Compound: 27; AM-0902	Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay	[PMID: 26942860]
CHO	IC₅₀	0.02 μM Compound: 27; AM-0902	Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced Ca2+ influx preincubated for 2 mins followed by AITC addition measured for 2 mins by Fluo-4 dye based FLIPR assay	[PMID: 26942860]
CHO	IC₅₀	0.071 μM Compound: 27; AM-0902	Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins Antagonist activity at rat TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins	[PMID: 26942860]
CHO	IC₅₀	0.131 μM Compound: 27; AM-0902	Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins Antagonist activity at human TRPA1 expressed in tetracycline-inducible T-REx expression system transfected CHO cells assessed as inhibition of AITC-induced 45Ca2+ uptake preincubated for 1 min followed by AITC addition measured after 12 mins	[PMID: 26942860]

In Vitro

AM-0902 is a potent, selective antagonist of TRPA1 with IC₅₀s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively. AM-0902 is highly permeable (average P_app=44.5 μcm/s in MDCK cells), an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells), and demonstrates good solubility (PBS pH 7.4: 226 μM, SIF: 248 μM). AM-0902 shows good selectivity over other TRP channels, as no activity is observed against human TRPV1 or TRPV4, or rat TRPV1, TRPV3, or TRPM8, at concentrations up to 10 μM. AM-0902 inhibits ⁴⁵Ca²⁺ flux upon activation of rat TRPA1 with methylglyoxal with an IC₅₀ of 0.019 μM^[1].

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

In Vivo

AM-0902 is a potent, selective antagonist of TRPA1 in vivo. AM-0902 has moderate terminal elimination half-life (t_1/2=0.6 h and 2.8 h for rat (0.5 mg/kg, iv), rat (30 mg/kg, oral)). A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902, with a significant reduction in flinching observed postdosing of 10 and 30 mg/kg. The unbound plasma concentrations (C_u) at 1 h for the 1, 3, 10, and 30 mg/kg doses are 0.051±0.024 (n=8), 0.19±0.11 (n=8), 0.58±0.35 (n=8), and 2.2±0.40 (n=8) μM, covering the in vitro rat TRPA1 ⁴⁵Ca²⁺ IC₅₀ at 0.72, 2.7, 8.2, and 30.3 fold, respectively. A good exposure-response relationship is observed in this target coverage model. An unbound in vivo IC₅₀ of 0.35 μM, which is in good agreement with the in vitro rat TRPA1 ⁴⁵Ca²⁺ IC₅₀, and unbound in vivo IC₉₀ of 1.7 μM are determined. It is noteworthy that at a dose of 30 mg/kg, AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC₉₀, making it a useful tool for exploration of in vivo models of acute pain^[1].

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

분자량

370.79

화학식

C₁₇H₁₅ClN₆O₂

CAS No.

1883711-97-4

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC2=NC(CCC3=CC=C(Cl)C=C3)=NO2)C=NC4=C1N(C)C=N4

선적

Room temperature in continental US; may vary elsewhere.

보관

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

용액&용해도

In Vitro:

DMSO : 150 mg/mL (404.54 mM; Need ultrasonic and warming; 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	2.6969 mL	13.4847 mL	26.9694 mL
5 mM	0.5394 mL	2.6969 mL	5.3939 mL
10 mM	0.2697 mL	1.3485 mL	2.6969 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, 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.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.73%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Schenkel LB, et al. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1)Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809. [Content Brief]

Cell Assay ^[1]	MDCK cells are generated and maintained for the TRPA1 calcium flux assays. On the day of assay, culture media is removed and cells are incubated for 10 min at room temperature (RT) with 50 μL of AM-0902 (compound 27) in AM-0902 dilution buffer [HBSS containing 1 mM HEPES+0.1 mg/mL BSA] at final concentrations (2.0 nM to 40 μM, 1:3 ratio), followed by another 3 min incubation at RT. The reaction mixture is aspirated, and cells are washed three times with phosphate buffer saline (PBS) containing 0.1 mg/mL BSA. Radioactivity is measured using a TopCount microplate scintillation counter. The activation of TRPA1 is measured by the cellular uptake of radioactive calcium^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[1]	Rats^[1] Rats are dosed orally with either vehicle (2% HPMC/1% Tween-80) or AM-0902 at 1, 3, 10, or 30 mg/kg. After 1 h, one left ventral hind paw is injected with the TRPA1 agonist AITC (0.1%). AM-0902 is also given by an intravenous (IV) injection to rats (0.5 mg/kg)^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. Schenkel LB, et al. Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1)Antagonists Demonstrating Potent in Vivo Activity. J Med Chem. 2016 Mar 24;59(6):2794-809. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6969 mL	13.4847 mL	26.9694 mL	67.4236 mL
	5 mM	0.5394 mL	2.6969 mL	5.3939 mL	13.4847 mL
	10 mM	0.2697 mL	1.3485 mL	2.6969 mL	6.7424 mL
	15 mM	0.1798 mL	0.8990 mL	1.7980 mL	4.4949 mL
	20 mM	0.1348 mL	0.6742 mL	1.3485 mL	3.3712 mL
	25 mM	0.1079 mL	0.5394 mL	1.0788 mL	2.6969 mL
	30 mM	0.0899 mL	0.4495 mL	0.8990 mL	2.2475 mL
	40 mM	0.0674 mL	0.3371 mL	0.6742 mL	1.6856 mL
	50 mM	0.0539 mL	0.2697 mL	0.5394 mL	1.3485 mL
	60 mM	0.0449 mL	0.2247 mL	0.4495 mL	1.1237 mL
	80 mM	0.0337 mL	0.1686 mL	0.3371 mL	0.8428 mL
	100 mM	0.0270 mL	0.1348 mL	0.2697 mL	0.6742 mL

AM-0902 Related Classifications

Neurological Disease Inflammation/Immunology

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:

AM-09021883711-97-4AM0902AM 0902TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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AM-0902

고객리뷰

Other Forms of AM-0902:

AM-0902 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

AM-0902 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

AM-0902 Related Classifications

Keywords:

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고객리뷰

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SAFETY DATA SHEET (SDS)

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