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Cat. No.: HY-101724

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ReN-1869 hydrochloride

Name: ReN-1869 hydrochloride
Brand: MedChemExpress
SKU: HY-101724
Availability: PreOrder

(Synonyms: NNC-05-1869 hydrochloride)

ReN 1869 hydrochloride is a novel, selective histamine H₁ receptor antagonist, which demonstrates affinity to the histamine H₁ receptor (guinea pig brain) with K_i of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with K_i of 0.45 μM.

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

CAS No.: 170149-76-5
Formula: C₂₄H₂₈ClNO₂
Molecular Weight:397.94

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

ReN-1869 hydrochloride Chemical Structure

CAS No.: 170149-76-5

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

IC₅₀ & Target

Ki: 0.19±0.04 μM (histamine H₁ receptor)^[1]

All Histamine Receptor Isoforms :

In Vitro

ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H₁ receptor antagonism. Binding studies with radioactively labelled ReN 1869 reveals high affinity only for the histamine H₁ receptor in addition to some affinity for a sigma site. ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels. ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [³H]pyrilamine) with a K_i of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [³H]1,3-di-tolylguanidine (DTG)] with a K_i of 0.45 μM. ReN 1869 dose-dependently reduces the responses with IC₅₀ of 1.70±0.002 μM^[1].

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

In Vivo

The in vivo binding of [³H]Mepyramine to mouse spinal cord and cerebellar histamine H₁ receptors is dose-dependently inhibited by ReN 1869. ReN 1869 (in doses as low as 10 μg/kg i.p.) significantly inhibits the histamine-evoked paw edema. The ED₅₀ is approximately 300 μg/kg. Interestingly, even a high dose of Mepyramine (10 mg/kg) is unable to inhibit significantly this type of edema (0.29±0.06 versus 0.34±0.05 in controls, n=7).ReN 1869 (1 mg/kg s.c.) is administered 30 min before paw injection with carrageenan and has no effect on the development of the paw edema. Dexamethasone (1 mg/kg s.c.) is given 1 h before carrageenan and expectedly diminished the edema. This effect is not affected by the simultaneous administration of 1 mg/kg ReN 1869^[1].

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

Chemical Information

CAS No. 170149-76-5
Molecular Weight 397.94
Formula C₂₄H₂₈ClNO₂
SMILES

O=C([C@H]1CN(CC/C=C2C3=CC=CC=C3CCC4=CC=CC=C\24)CCC1)O.[H]Cl
Synonyms

NNC-05-1869 hydrochloride
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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)

References

[1]. Olsen UB, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. [Content Brief]

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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.

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100 mg

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