2. GPCR/G Protein
  3. Adenosine Receptor
  4. MRS7469

MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields.

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MRS7469

MRS7469 Chemical Structure

CAS No. : 2257428-48-9

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MRS7469 Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields[1][2][3].

IC50 & Target[1]

hA1AR

2.14 nM (Kd)

In Vitro

MRS7469 exhibits high binding affinity for hA1AR (pKi=8.67) and mA1AR (pKi=9.43), while its affinity for hA2AAR, hA3AR and mA3AR is much lower[2].
MRS7469 exhibits a binding affinity of 2.14 nM for targeting hA1AR, with over 2000-fold selectivity over other adenosine receptor subtypes[3].

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

MRS7469 Related Antibodies
In Vivo

When administered peripherally, MRS7469 (52 μg/kg; intracerebroventricular injection) preferentially activates central A1 adenosine receptors rather than peripheral A3 adenosine receptors, inducing A1 adenosine receptor-dependent hypothermia and motor inhibition; it also causes severe hypothermia[2].

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

Animal Model: Mice[2]
Dosage: 52 µg/kg (i.c.v.)
Administration: i.c.v.
Result: Induced intense hypothermia.
Activated central A1 adenosine receptors preferentially over peripheral A3 adenosine receptors, leading to A1 adenosine receptor-dependent hypothermia and locomotor depression.
Exhibited a high affinity for mouse A1 adenosine receptors (Ki=0.37 nM).
Crossed the blood-brain barrier sufficiently to activate central A1 adenosine receptors.
Molecular Weight

433.93

Formula

C21H28ClN5O3
CAS No.
SMILES

OC[C@]12[C@]([C@@H](N3C4=NC(Cl)=NC(NC(C5CCC5)C6CCC6)=C4N=C3)[C@@H]([C@@H]2O)O)([H])C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MRS7469 Related Classifications

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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:

MRS74692257428-48-9MRS 7469MRS-7469Adenosine ReceptorP1 receptorA2AARadenosine receptor subtypesmolecular dynamics simulationA1ARA1 adenosine receptorlocomotor depressionhypothermiapsychomotor dysfunctionblood-brain barrierdepressionInhibitorinhibitorinhibit

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