Aminopicoline (Synonyms: Ascensil; 2-Amino-4-methylpyridine)

Name: Aminopicoline
Brand: MedChemExpress
SKU: HY-W003969
Rating: 4.5 (1 reviews)

Cat. No.: HY-W003969 Purity: 99.99%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Aminopicoline (Ascensil) is a potent and non-selective inhibitor of nitric oxide synthase (NOS) isoenzymes (iNOS, nNOS, eNOS). Aminopicoline competes with arginine at the substrate-binding site of nitric oxide synthase, reduces cellular nitric oxide production, inhibits the elevation of plasma nitrate, increases mean arterial pressure at high doses, and also serves as a basis for radiolabeled ligands to localize nitric oxide synthase binding sites. Aminopicoline can be used in the research of diseases associated with septic shock, joint inflammation, intestinal inflammation, and CNS inflammation.

For research use only. We do not sell to patients.

Aminopicoline Chemical Structure

CAS No. : 695-34-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
25 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Aminopicoline:

Aminopicoline (Standard) Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All NO Synthase Isoform Specific Products:

View All Isoforms

nNOS iNOS eNOS

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

eNOS

iNOS

nNOS

In Vitro

Aminopicoline (range of concentrations; 45-60 min at 37 °C) acts as a potent, nonselective, arginine-competitive inhibitor of human iNOS, nNOS, and eNOS, with IC₅₀ values ranging from 50 to 62 nM, and a K_i value of 76 nM for human iNOS^[1].
³H]aminopicoline (range of concentrations; 45-60 min at 37 °C) binds with high, nonselective affinity to human iNOS, nNOS, and eNOS, with K_d values of 59, 111, and 136 nM, respectively, and binding is independent of NADPH presence^[1].
Aminopicoline (range of concentrations; 45-60 min at 37 °C) competitively inhibits binding of [³H]aminopicoline to human iNOS, nNOS, and eNOS, with K_i values of 55, 65, and 98 nM, respectively, consistent with saturation binding results^[1].
Aminopicoline (1-1000 nM; 60 min at 30 °C during enzyme activity assay) potently inhibits murine NOS II with an IC₅₀ of 6 nM, with reduced potency against recombinant human NOS II (IC₅₀ = 40 nM) and recombinant human NOS I and NOS III (IC₅₀ = 100 nM), via a competitive mechanism with L-arginine^[2].
Aminopicoline (0.3-10 μM; 20 h, simultaneous addition with LPS/interferon-γ) inhibits nitrite production in LPS/interferon-γ-stimulated RAW 264.7 cells with an IC₅₀ of 1.5 ± 0.3 μM by directly inhibiting NOS II catalytic activity without affecting NOS II protein induction or arginine uptake, with potency reduced by increased extracellular arginine concentrations^[2].

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

In Vivo

Aminopicoline (0.009-20.8 mg/kg; i.v., continuous infusion for 1 hour; s.c., single dose; p.o., single dose) potently inhibits LPS-induced systemic NOS II activity in conscious rats with a 6.9× selectivity for NOS II over NOS III, and is active via intravenous, subcutaneous, and oral routes with ID₅₀ values of 0.009 mg kg⁻¹ min⁻¹, 0.3 mg/kg, and 20.8 mg/kg, respectively^[2].

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

Animal Model:	Wistar (male, 250-300 g; systemic inflammation model induced by LPS)^[2]
Dosage:	0.009 mg kg⁻1 min⁻1 (i.v., LPS-induced nitrate elevation ID50); 0.060 mg kg⁻1 min⁻1 (i.v., mean arterial pressure ED50); 0.3 mg/kg (s.c., LPS-induced nitrate elevation ID50); 20.8 mg/kg (p.o., LPS-induced nitrate elevation ID50)
Administration:	i.v., continuous infusion for 1 hour; s.c., single dose; p.o., single dose
Result:	Inhibited LPS-induced plasma nitrate elevation by 50% (ID50) at 0.009 mg kg⁻1 min⁻1 i.v..\nIncreased mean arterial pressure by 50% (ED50) in untreated rats at 0.060 mg kg⁻1 min⁻1 i.v..\nAchieved 6.9× selectivity for NOS II over NOS III in vivo.\nInhibited LPS-induced plasma nitrate elevation by 50% (ID50) at 0.3 mg/kg s.c..\nInhibited LPS-induced plasma nitrate elevation by 50% (ID50) at 20.8 mg/kg p.o..

Molecular Weight

108.14

Formula

C₆H₈N₂

CAS No.

695-34-1

Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=CC(C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (924.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (462.36 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	9.2473 mL	46.2364 mL	92.4727 mL
5 mM	1.8495 mL	9.2473 mL	18.4945 mL
10 mM	0.9247 mL	4.6236 mL	9.2473 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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 (23.12 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 (23.12 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 (23.12 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.99%

Select Batch:

Data Sheet (276 KB) SDS (642 KB)

COA (248 KB) HNMR (129 KB) GC (177 KB)

Handling Instructions (2659 KB)

References

[1]. Boer R, et al. The inhibitory potency and selectivity of arginine substrate site nitric-oxide synthase inhibitors is solely determined by their affinity toward the different isoenzymes. Mol Pharmacol. 2000;58(5):1026-1034. [Content Brief]

[2]. Faraci WS, et al. 2-Amino-4-methylpyridine as a potent inhibitor of inducible NO synthase activity in vitro and in vivo. Br J Pharmacol. 1996;119(6):1101-1108. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	9.2473 mL	46.2364 mL	92.4727 mL	231.1818 mL
	5 mM	1.8495 mL	9.2473 mL	18.4945 mL	46.2364 mL
	10 mM	0.9247 mL	4.6236 mL	9.2473 mL	23.1182 mL
	15 mM	0.6165 mL	3.0824 mL	6.1648 mL	15.4121 mL
	20 mM	0.4624 mL	2.3118 mL	4.6236 mL	11.5591 mL
	25 mM	0.3699 mL	1.8495 mL	3.6989 mL	9.2473 mL
	30 mM	0.3082 mL	1.5412 mL	3.0824 mL	7.7061 mL
	40 mM	0.2312 mL	1.1559 mL	2.3118 mL	5.7795 mL
	50 mM	0.1849 mL	0.9247 mL	1.8495 mL	4.6236 mL
	60 mM	0.1541 mL	0.7706 mL	1.5412 mL	3.8530 mL
	80 mM	0.1156 mL	0.5780 mL	1.1559 mL	2.8898 mL
	100 mM	0.0925 mL	0.4624 mL	0.9247 mL	2.3118 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Aminopicoline Related Classifications

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.

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Aminopicoline (Synonyms: Ascensil; 2-Amino-4-methylpyridine)

Customer Review

Other Forms of Aminopicoline:

Aminopicoline Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All NO Synthase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Aminopicoline Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Aminopicoline Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report