SQ 20858
SQ 20858 is a competitive Angiotensin-converting enzyme inhibitor. SQ 20858 blocks the conversion of Angiotensin I to Angiotensin II, inhibits the inactivation of Bradykinin (HY-P0206) and amplifies the hypotensive response of Bradykinin. SQ 20858 blocks the pressor responses of Angiotensin I and rabbit Renin, but has no effect on the pressor effect of angiotensin II . SQ 20858 reduces blood pressure in renal hypertension models. SQ 20858 can be used in studies related to chronic renal hypertension.
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- CAS No.: 35115-62-9
- Formule: C57H77N15O14
- Masse moléculaire:1196.31
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
SQ 20858 (0.4-20 mg/100 g; subcutaneous injection; once every two weeks) administered via subcutaneous injection at the highest dose of 20 mg/100 g does not alter the systolic blood pressure of normotensive Sprague Dawley rats[1].
SQ 20858 (36 mg/kg; 60-minute infusion) exerts a significant, rapid and transient hypotensive effect in rabbits with the transitional one-kidney Goldblatt hypertension model, reducing the mean blood pressure to a nadir of 94/64 mmHg, which returns to the baseline level within 24 hours[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley (male, initial weight 120 gm, renal hypertension model via bipolar kidney ligation followed by contralateral nephrectomy)[1]
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Dosage:0.4 mg/100 g; 0.8 mg/100 g; 20 mg/100 g
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Administration:s.c.; biweekly; 10 doses (0.4 mg/100 g); 5 doses (0.8 mg/100 g); 4 doses (20 mg/100 g)
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Result:Lowered mean systolic pressure from 184 mmHg to 177 mmHg after 10 doses of 0.4 mg/100 g.
Lowered mean systolic pressure to 168 mmHg after 5 doses of 0.8 mg/100 g.
Lowered mean systolic pressure to 160 mmHg (statistically significant, P < .001) after 4 doses of 20 mg/100 g, with the effect remaining until sacrifice 2 weeks later.
Showed no statistically significant difference in mean heart weight compared to normotensive controls (0.794 gm vs 0.784 gm at week 35; 0.797 gm vs 0.787 gm combined).
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Animal Model:New Zealand white male rabbits (1.8-2.0 kg body weight; chronic one-kidney Goldblatt hypertension model)[2]
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Dosage:36 mg/kg
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Administration:Infused over 60 minutes
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Result:Produced no decline in mean blood pressure from baseline 128/98 mmHg.
Chemical Information
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CAS No. 35115-62-9
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Masse moléculaire 1196.31
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Formule C57H77N15O14
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SMILES
O=C(N1[C@@H](CCC1)C(N[C@@H](CC2=CN=CN2)C(N3[C@@H](CCC3)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@@H](C)CC)C(N4[C@@H](CCC4)C(N5[C@@H](CCC5)C(O)=O)=O)=O)=O)=O)=O)=O)[C@@H](NC([C@H](CC(N)=O)NC([C@@H]6CCC(N6)=O)=O)=O)CC7=CNC8=CC=CC=C78
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Sequence
{Pyr}-Asn-Trp-Pro-His-Pro-Gln-Ile-Pro-Pro
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Sequence Shortening
{Pyr}-NWPHPQIPP
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Loyke H F. Dose response of SQ 20,858 in chronic renal hypertension[J]. Pharmacological Research Communications, 1977, 9(2): 181-186. [Content Brief]
[2]. Romero JC, et al. Effect of blockade of angiotensin-I converting enzyme on the blood pressure of renal hypertensive rabbits. Cardiovasc Res. 1974 Sep;8(5):681-7. [Content Brief]
[3]. Murthy VS, et al. Inhibition of angiotensin converting enzyme by SQ 14,225 in conscious rabbits. European journal of pharmacology. 1977 Dec 01;46(3):207-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SQ 20858 Related Classifications
HY-P2225 Related Classifications
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