2. Cytoskeleton TGF-beta/Smad Stem Cell/Wnt
  3. Integrin TGF-beta/Smad
  4. MORF-627

MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety.

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

MORF-627

MORF-627 Chemical Structure

CAS No. : 2412688-16-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

MORF-627 Related Antibodies

Top Publications Citing Use of Products

View All Integrin Isoform Specific Products:

View All Isoforms
αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety[1][2][3].

IC50 & Target[1]

αvβ6

1.1 nM (IC50)

In Vitro

MORF-627 potently and selectively inhibits purified human integrin αvβ6 with an IC50 of 1.1 nM, exhibiting 450-fold and 300-fold selectivity over αvβ1 and αvβ8, respectively[1].
MORF-627 inhibits the binding of proTGF-β1 to HEK293 cells overexpressing human αvβ6, with an IC50 of 9.2 nM[1].
MORF-627 potently inhibits αvβ6-mediated TGF-β1 activation in a cell co-culture system, with an IC50 of 2.63 nM after 24 h of treatment[1].
MORF-627 inhibits the mRNA expression of ECM proteins in a co-culture system of primary fibroblasts and epithelial cells derived from human idiopathic pulmonary fibrosis (IPF)[1].
MORF-627 (0.01-3 μM; 3 d) induces dose-dependent proliferation of primary human bladder epithelial cells, while co-administration of 5 ng/mL exogenous TGF-β1 reverses this effect[3].
MORF-627 (0.01-3 μM; 3 d) induces dose-dependent proliferation of primary human alveolar epithelial cells within 3 days, and this effect is reversed by co-administration of 5 ng/mL exogenous TGF-β1[3].

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

MORF-627 Related Antibodies

Real Time qPCR[1]

Cell Line: coculture of human primary epithelial cells expressing αvβ6 and human IPF fibroblasts
Concentration: dose range
Incubation Time: 72 h
Result: Inhibited COL1A1 mRNA expression with an IC50 of 1.8 nM.
Inhibited COL3A1 mRNA expression with an IC50 of 12.8 nM.
Inhibited FN mRNA expression with an IC50 of 20.3 nM.
Parmacokinetics
Species Dose Route CL Vss T1/2 AUC0-inf Cmax Tmax F
Mice[1] 1 mg/kg i.v. 18.0 mL/min/kg 2.07 L/kg 1.9 h 0.94 μg·h/mL / / /
Rat[1] 1 mg/kg i.v. 27.6 mL/min/kg 3.08 L/kg 1.9 h 0.61 μg·h/mL / / /
Dog[1] 1 mg/kg i.v. 9.53 mL/min/kg 1.84 L/kg 4.9 h 2.97 μg·h/mL / / /
Cynomolgus Monkey[1] 1 mg/kg i.v. 10.5 mL/min/kg 2.45 L/kg 4.9 h 1.59 μg·h/mL / / /
Mice[1] 30 mg/kg p.o. / / 2.6 h 19 7.6 μg/mL 0.25 h 66 %
Rat[1] 30 mg/kg p.o. / / 1.8 h 14 14 μg/mL 0.25 h 74 %
Cynomolgus Monkey[1] 5 mg/kg p.o. / / 4.8 h 1.6 μg·h/mL 0.54 μg/mL 1.0 h 16 %
In Vivo

MORF-627 (0.1-100 mg/kg; p.o.; twice daily; for 3 consecutive days) dose-dependently inhibits the αvβ6-mediated TGF-β signaling pathway (detected by reduced pSMAD2 levels) in a bleomycin (HY-108345)-induced acute mouse pulmonary fibrosis model, with an in vivo IC50 of approximately 8.3 nM[1].
MORF-627 (1-10 mg/kg; p.o.; twice daily; for 14 consecutive days) reduces fibrosis severity and collagen deposition in a bleomycin-induced chronic mouse model of pulmonary fibrosis[1].
MORF-627 induces epithelial proliferative changes in the bladder of 33% of tested cynomolgus macaques 28 days after administration[2].
MORF-627 (administered via gavage; daily; for consecutive 28 days at 30-180-120 mg/kg/day) induces dose-related proliferation of bladder epithelial cells; 33% of treated cynomolgus monkeys develop early invasive urothelial carcinoma, and the Ki67 proliferation index of urothelial cells is significantly increased in all dose groups[3].

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

Animal Model: C57BL/6J (male, 7 weeks old, bleomycin-induced chronic model)[1]
Dosage: 1-10 mg/kg
Administration: p.o.; twice daily; 14 days
Result: Produced a statistically significant 33% reduction in the Modified Ashcroft Score compared to vehicle controls at 1 mg/kg, 3 mg/kg, and 10 mg/kg doses.
Significantly reduced total collagen deposition by 31%, decreased collagen fiber density, and reduced the collagen structure index compared to vehicle controls at 3 mg/kg dose.
Showed a trend toward reduced Picro Sirius Red positive area, which did not reach statistical significance.
Animal Model: Macaca fascicularis (2-5 years of age, 2.7-4.3 kg, both sexes, mainland Asia origin)[3]
Dosage: 30 mg/kg/day; 60 mg/kg/day; 180/120 mg/kg/day (initial 3 days at 180 mg/kg/day, then 25 days at 120 mg/kg/day)
Administration: oral gavage; daily; 28 days
Result: Induced early-stage invasive urothelial carcinoma in 2 of 6 monkeys at 180/120 mg/kg/day.
Showed significantly increased urothelial cell proliferation, with Ki67 scores of 48 and 49 positive nuclei per 1000 urothelial cells in monkeys with tumors at 180/120 mg/kg/day, and Ki67 scores of 55 and 17 positive nuclei per 1000 urothelial cells in one male and one female monkey at 30 mg/kg/day, respectively.
Reached mean steady-state plasma Cmax levels (total) of 2.6 μM on day 28 at 30 mg/kg/day and 7.8 μM on day 28 at 120 mg/kg/day, exceeding the integrin αvβ6 cellular IC50.
Caused no treatment-related clinical signs, body weight changes, or food consumption effects at 30, 60, or 120 mg/kg/day.
Molecular Weight

537.67

Formula

C31H40FN3O4
CAS No.
SMILES

OC([C@@H](N1C[C@@H](CC1)OCCCCC(N2)=CC=C3C2=NCCC3)C4=C(C=CC(F)=C4)[C@@H]5CCC6(CO5)CC6)=O
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

MORF-627 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MORF-6272412688-16-3MORF627MORF 627IntegrinTGF-beta/SmadTransforming growth factor betaearly-stage invasive urothelial carcinomaidiopathic pulmonary fibrosiscynomolgus macaquesintegrin αvβ6epithelial-to-mesenchymal transitionpSMAD2TGF-β1collagen depositionhuman bladder epithelial cellsextracellular matrixInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MORF-627
Cat. No.:
HY-149136
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.