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Referencia número: HY-153690

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Progranulin modulator-1

Progranulin modulator-1 (Compound 60) is an orally active enhancer of progranulin (PGRN) secretion. Progranulin modulator-1 enhances the potency of BV-2 cell to increase PGRN levels, has inhibitory effect on hERG and Low cytotoxicity, the PGRN EC₅₀ and hERG IC₅₀ were 83 and 3100 nM, respectively.

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No. CAS: 2641013-11-6
Fòrmula: C₂₁H₂₁F₂N₃O
Peso molecular:369.41

Almacenamiento:

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

Data Sheet (274 KB)

Progranulin modulator-1 Chemical Structure

No. CAS: 2641013-11-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
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Actividad biológica

Descripciòn

IC₅₀ & Target

EC50: 83 nM (PGRN); IC50: 3100 nM (hERG)

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Cellular Effect

Cell Line	Type	Value	Description	References
BV-2	EC₅₀	83 nM Compound: 60	Induction of progranulin secretion in mouse BV-2 cells Induction of progranulin secretion in mouse BV-2 cells	[PMID: 36368496]

In Vitro

Progranulin modulator-1 (Compound 60) has an efflux ratio (ER) value <2, indicating that it is not a substrate for MDR and shows high brain tissue binding and high metabolic stability^[1].
Progranulin modulator-1 In vitro ADME properties for selected molecules^[1]

MDCK-MDR1 P_appA→B[ER]	Protein Binding, _Fu	Brain Tissue Binding, _Fu	Hepatocytes t_1/2 , CL_int
0.53 [1.11]	3.1 (m); 5.5 (h)	0.9 (m)	>120, <68.2 (m); >120, <14.7 (h)

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

In Vivo

Progranulin modulator-1 (Compound 60) (i.v.: 1 mg/kg, p.o.: 10 mg/kg) has good mouse PK profiles, with high bioavailability and half-life, oral availability up to 99% and shows K_puu > 1, indicating very favorable enrichment of in brain at 8 h post dosing, achieve a progranulin modulating effect with a relatively low dosage of Progranulin modulator-1^[1].
Pharmacokinetic Parameters for Progranulin Modulator-1 in Mouse^[1]

PO t_1/2 (h)	IV t_1/2 (h)	C_max,u (nM)	K_puu @ 8 h	F (%)	CL	V_dss
4.8	7.4	62	2.91	99	2.08	15.2

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

Chemical Information

No. CAS 2641013-11-6
Peso molecular 369.41
Fòrmula C₂₁H₂₁F₂N₃O
SMILES

FC1=CC=C(C=C1)[C@@H]2N(C3=N[C@H](C4(CNC4)F)CO3)CCC5=CC=CC=C52
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Peng X, et al. Discovery of oxazoline enhancers of cellular progranulin release. Bioorg Med Chem Lett. 2023 Jan 15;80:129048. [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.

Keywords

Progranulin modulator-1

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Actividad biológica
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- In Vitro
- In Vivo
Chemical Information
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Progranulin modulator-1

Ver todos los productos específicos de isoformas TNF Receptor

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Progranulin modulator-1 Related Classifications

HY-153690 Related Classifications