Art. -Nr.: HY-106432A

Sabcomeline hydrochloride

(Synonyms: SB-202026 hydrochloride; Memric hydrochloride)

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Sabcomeline (SB-202026; Memric) hydrochloride is a muscarinic receptor agonist capable of crossing the blood-brain barrier. Sabcomeline hydrochloride exhibits affinity for all hM1 to hM5 subtypes (pK_i=6.72-7.23), and shows near-full agonism at the hM3 receptor, inducing extracellular acidification. Sabcomeline hydrochloride alters the binding kinetics of dopamine D2 receptors through neural network regulation. Sabcomeline hydrochloride also causes minimal cardiovascular changes, effectively reverses spatial memory deficits in rodents and induces conditioned taste aversion. Sabcomeline hydrochloride is an important tool compound in studies of Alzheimer's disease and related neurodegenerative diseases.

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Reinheit: 99.81%
CAS. Nr.: 159912-58-0
Formel: C₁₀H₁₆ClN₃O
Molecular Weight:229.71

Speicherung:

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Sabcomeline hydrochloride Chemical Structure

CAS. Nr.: 159912-58-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

mAChR1

6.72 (pKi)

mAChR3

7.03 (pKi)

mAChR4

7.23 (pKi)

mAChR5

7.14 (pKi)

Alle mAChR Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Compared with Carbamoylcholine (HY-B1208), Sabcomeline hydrochloride exhibits the lowest potency (≈20%) at the hM₁ and hM₅ subtypes; moderate potency at the hM₄ (≈38%) and hM₂ (≈57%) subtypes; and the highest partial agonist potency (≈70%) at the hM₃ subtype^[1].

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

In Vivo

Sabcomeline hydrochloride (0.01-3 mg/kg; i.v.; 0.3 mg/kg; i.p.) exhibits dose-dependent, non-M₁-selective mACh receptor binding in mouse brain and heart with rapid dissociation (return to control levels by 3-4 hours post-0.3 mg/kg i.v. dose), and alters striatal dopamine D₂ receptor binding kinetics by decreasing [³H]NMSP k₃ by ~15% and increasing [³H]raclopride BP by ~20%^[2].
Sabcomeline hydrochloride (0.03-0.1 mg/kg; i.p.; single dose 15 minutes prior to testing) significantly reverses 20-s delay-induced T-maze choice accuracy deficits in male Hooded Lister rats, with cholinergic side effects appearing at higher doses of 0.3 mg/kg and above^[3].
Sabcomeline hydrochloride (0.3-1.0 mg/kg; i.p.; single dose 15 minutes after saccharin exposure) induces significant conditioned taste aversion in male Hooded Lister rats at a minimum effective dose of 0.3 mg/kg, with 60% inhibition of saccharin intake observed at 1.0 mg/kg^[3].

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

Animal Model:

ddY mice (male, 8-9 weeks old)^[2]
Dosage:

0.01-3 mg/kg (i.v.); 0.3 mg/kg (i.p.)
Administration:

i.v.; i.p. (single dose 30 minutes before tracer injection)
Result:

Inhibited specific [³H]NMPB binding in cerebral cortex, striatum, and hippocampus with an estimated IC₅₀ of ~0.2 mg/kg.
Reached maximum muscarinic acetylcholine (mACh) receptor occupancy 1 hour after intravenous injection of 0.3 mg/kg, with binding availability returning to control levels by 3-4 hours.
Dose-dependently inhibited specific [³H]QNB binding in the heart.
Decreased the forward rate constant (k₃) of [³H]NMSP binding in the striatum by approximately 15%.
Decreased both the forward rate constant (k₃) and reverse rate constant (k₄) of [³H]raclopride binding in the striatum.
Increased the [³H]raclopride binding potential (BP=k₃/k₄) in the striatum by approximately 20%.

Animal Model:

ddY mice (male, 8-9 weeks old)^[2]
Dosage:

0.01-3 mg/kg
Administration:

i.v.
Result:

Showed a strong correlation between mACh receptor occupancy values measured 30 minutes and 60 minutes after tracer injection in the cerebral cortex, hippocampus, and striatum.

Animal Model:

Hooded Lister rats (male)^[3]
Dosage:

0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
Administration:

i.p.; single dose 15 minutes after saccharin exposure
Result:

Induced significant conditioned taste aversion at minimum effective dose of 0.3 mg/kg (P < 0.05).
Inhibited saccharin consumption by 60% compared to vehicle controls at 1.0 mg/kg, with slight diarrhoea observed.
Failed to produce significant reduction in saccharin intake at 0.03 mg/kg and 0.1 mg/kg.

Chemical Information

CAS. Nr. 159912-58-0
Appearance Solid
Molecular Weight 229.71
Formel C₁₀H₁₆ClN₃O
Color White to off-white
SMILES

CO/N=C([C@@H]1C2CCN(CC2)C1)\C#N.Cl
Synonyms

SB-202026 hydrochloride; Memric hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 125 mg/mL (544.16 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3533 mL

21.7666 mL

43.5331 mL

5 mM

0.8707 mL

4.3533 mL

8.7066 mL

10 mM

0.4353 mL

2.1767 mL

4.3533 mL

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 (stored under nitrogen, away from moisture). 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

Verweise

[1]. Wood M D, et al. Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry[J]. British journal of pharmacology, 1999, 126(7): 1620.

[2]. Hosoi R, et al. Effect of sabcomeline on muscarinic and dopamine receptor binding in intact mouse brain. Ann Nucl Med. 2003;17(2):123-130. [Content Brief]

[3]. Hatcher JP, et al. Sabcomeline (SB-202026), a functionally selective M1 receptor partial agonist, reverses delay-induced deficits in the T-maze. Psychopharmacology (Berl). 1998;138(3-4):275-282. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	4.3533 mL	21.7666 mL	43.5331 mL	108.8329 mL
	5 mM	0.8707 mL	4.3533 mL	8.7066 mL	21.7666 mL
	10 mM	0.4353 mL	2.1767 mL	4.3533 mL	10.8833 mL
	15 mM	0.2902 mL	1.4511 mL	2.9022 mL	7.2555 mL
	20 mM	0.2177 mL	1.0883 mL	2.1767 mL	5.4416 mL
	25 mM	0.1741 mL	0.8707 mL	1.7413 mL	4.3533 mL
	30 mM	0.1451 mL	0.7256 mL	1.4511 mL	3.6278 mL
	40 mM	0.1088 mL	0.5442 mL	1.0883 mL	2.7208 mL
	50 mM	0.0871 mL	0.4353 mL	0.8707 mL	2.1767 mL
	60 mM	0.0726 mL	0.3628 mL	0.7256 mL	1.8139 mL
	80 mM	0.0544 mL	0.2721 mL	0.5442 mL	1.3604 mL
	100 mM	0.0435 mL	0.2177 mL	0.4353 mL	1.0883 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.

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Sabcomeline hydrochloride

MCE Bioactive Compound Library

Alle mAChR Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sabcomeline hydrochloride Related Classifications

HY-106432A Related Classifications