PARP7-IN-27
PARP7-IN-27 is a blood-brain barrier-permeable and selective PARP7 inhibitor with an IC50 of 22.8 nM. PARP7-IN-27 alleviates neuroinflammation and astrocyte activation, mitigates autophagy-related alterations, reduces the levels of ischemia-associated pro-inflammatory factors, and maintains the expression of synaptic markers. PARP7-IN-27 can be used in studies related to ischemic stroke.
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- CAS No.: 3051563-45-9
- 화학식: C15H11F4N3O2
- 분자량:341.26
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
PARP7 22.8 nM (IC50) |
TNF-α |
IL-6 |
ULK1 |
In Vitro
PARP7-IN-27 (compound B-6) exhibits potent inhibitory activity against the PARP7 enzyme (IC50 = 22.8 nM), shows moderate selectivity for PARP10 (selectivity index = 4.7) and PARP14 (selectivity index = 5.3), and possesses higher selectivity for the remaining PARP family subtypes; it exerts a weak inhibitory effect on the hERG channel (IC50 = 27.45 μM)[1].
PARP7-IN-27 exhibits good Caco-2 cell permeability, with a Papp A-to-B value of 31.09 ×10-6 cm/s and an efflux ratio of 0.62[1].
PARP7-IN-27 (1‑4 μM) downregulates GFAP protein levels, reduces ULK1 expression, and decreases the LC3B‑II/LC3B‑I ratio in primary mouse astrocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-∞ | Vz | CL | B/P |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.29 h | 0.08 h | 1963.08 ng/mL | 954.23 ng·h/mL | 901.07 mL/kg | 2122.64 mL/h/kg | 63.7 % |
In Vivo
PARP7-IN-27 (2.07 mg/kg; i.v.; single dose) retains substantial anti-ischemic activity when dosing is delayed up to 12 hours after ischemic onset in the rat tMCAO model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 180-200 g, transient middle cerebral artery occlusion ischemic stroke model)[1]
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Dosage:0.69, 2.07, 6.21 mg/kg (24h acute infarct assessment)
2.07, 6.21 mg/kg (inflammatory evaluation)
2.07, 6.21 mg/kg (sensorimotor functional recovery) -
Administration:i.v. (single dose immediately post reperfusion) (acute infarct assessment)
i.v. (qd for 3 days starting 1 hour post reperfusion) (inflammatory evaluation)
i.v. (qd for 14 days starting 1 hour post reperfusion) -
Result:Reduced residual infarct volume to 9.00% at 0.69 mg/kg, 7.60% at 2.07 mg/kg, and 6.80% at 6.21 mg/kg, compared to 29.20% baseline infarct volume in the untreated model group.
Reduced Longa neurological deficit scores, decreased peri-infarct TNF-α and IL-6 levels, reduced elevated GFAP expression, and partially restored levels of synaptic markers PSD-95 and synaptophysin.
Reduced foot-fault ratio in the grid walking test, ameliorated forelimb use asymmetry in the cylinder test, shortened adhesive removal time, and improved striatal histopathological morphology over the 21-day observation period.
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Animal Model:Sprague-Dawley rats (male, 180-200 g, transient middle cerebral artery occlusion ischemic stroke model)[1]
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Dosage:2.07 mg/kg
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Administration:i.v.; single dose administered immediately after reperfusion following 1, 3, 6, 12, or 18 hours of occlusion
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Result:Retained robust neuroprotective effect at 6 hours post occlusion, clearly preserved anti-ischemic activity at 12 hours post occlusion, and showed reduced efficacy after 18 hours of occlusion.
Chemical Information
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CAS No. 3051563-45-9
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분자량 341.26
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화학식 C15H11F4N3O2
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SMILES
O=C1C(C(F)(F)F)=C(N2CC(C(C3=CC=C(F)C=C3)=O)C2)C=NN1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP7-IN-27 Related Classifications
HY-189217 Related Classifications
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