ELN 441958

Product Name: ELN 441958
CAS No.: 913064-47-8
Chemical Name: ELN 441958
Synonyms: CS-1805;ELN 441958;7-chloro-2-[3-(9-pyridin-4-yl-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl]-3H-isoindol-1-one;7-Chloro-2-[3-[[9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecan-3-yl]carbonyl]phenyl]-2,3-dihydroisoindol-1-one;1H-Isoindol-1-one, 7-chloro-2,3-dihydro-2-[3-[[9-(4-pyridinyl)-3,9-diazaspiro[5.5]undec-3-yl]carbonyl]phenyl]-;7-chloro-2-[3-(9-pyridin-4-yl-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl]-3H-isoindol-1-one ELN441958;low CNS exposure,ELN-441958,Inhibitor,anti-hyperalgesic,ELN441958,Bradykinin Receptor,inhibit,high oral bioavailability
CBNumber: CB82627797
Molecular Formula: C29H29ClN4O2
Formula Weight: 501.02
MOL File: 913064-47-8.mol

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ELN 441958 Property

Boiling point:: 738.4±60.0 °C(Predicted)
Density: 1.37±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: Soluble in DMSO
form: Powder
pka: 10.87±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-4807
Product name: ELN-441958
Purity: 99.84%
Packaging: 5mg
Price: $420
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0013895
Product name: ELN-441958
Purity: 95.00%
Packaging: 5MG
Price: $503.35
Updated: 2021/12/16

ApexBio Technology

Product number: B5925
Product name: ELN441958
Packaging: 5mg
Price: $551
Updated: 2021/12/16

ChemScene

Product number: CS-4807
Product name: ELN-441958
Purity: 99.84%
Packaging: 10mg
Price: $600
Updated: 2021/12/16

ChemScene

Product number: CS-4807
Product name: ELN-441958
Purity: 99.84%
Packaging: 50mg
Price: $1800
Updated: 2021/12/16

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ELN 441958 Chemical Properties,Usage,Production

Biological Activity

eln441958 is a novel, potent and selective bradykinin b1 receptor antagonist with ki value of 0.26 nm [1].the bradykinin b1 receptor is a g-protein coupled receptor with principal ligand of bradykinin and plays an important role in chronic pain and inflammation [1].eln441958 is a novel, potent and selective bradykinin b1 receptor antagonist. in imr-90 lung fibroblast cell membranes, eln441958 competitively inhibited the binding of the agonist [3h]dakd to the human b1 receptor with ki value of 0.26 nm. in imr-90 cells expressing the native human b1 receptor, eln441958 concentration-dependently antagonized calcium mobilization induced by dakd with kb value of 0.12 nm. eln441958 is highly selective for b1 over b2 receptors. eln441958 failed to inhibit the calcium mobilization induced by b2-receptor agonist bk. eln441958 also inhibited human μ-, δ-, κ- opioid receptors and muscarinic m1 receptor with ki values of 0.13, 0.69, 1.5 and 0.37 μm, respectively. eln441958 is also an agonist at the δ-opioid receptor (ec50 = 0.76 μm) and μ-opioid receptor. in vitro, eln441958 exhibited good permeability and metabolic stability [1].in rats and rhesus monkeys, eln441958 exhibited high oral bioavailability and moderate plasma half-lives. in rhesus monkeys, eln441958 dose-dependently reduced the thermal hyperalgesia induced by carrageenan with ed50 value of ~3 mg/kg s.c [1].

References

[1]. hawkinson je, szoke bg, garofalo aw, et al. pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin b1 receptor antagonist eln441958, j pharmacol exp ther, 2007, 322(2): 619-630.

ELN 441958 Preparation Products And Raw materials

Raw materials

Preparation Products

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ELN 441958 Suppliers

China 48 United States 11 Global 59

MedChemexpress LLC

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913064-47-8, ELN 441958Related Search:

7-chloro-2-[3-(9-pyridin-4-yl-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl]-3H-isoindol-1-one

7-Chloro-2-[3-[[9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecan-3-yl]carbonyl]phenyl]-2,3-dihydroisoindol-1-one

ELN 441958

7-chloro-2-[3-(9-pyridin-4-yl-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl]-3H-isoindol-1-one ELN441958

CS-1805

1H-Isoindol-1-one, 7-chloro-2,3-dihydro-2-[3-[[9-(4-pyridinyl)-3,9-diazaspiro[5.5]undec-3-yl]carbonyl]phenyl]-

low CNS exposure,ELN-441958,Inhibitor,anti-hyperalgesic,ELN441958,Bradykinin Receptor,inhibit,high oral bioavailability

913064-47-8

C29H29ClN4O2

Inhibitors